naphthoquinones

Summary

Summary: Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.

Top Publications

  1. ncbi YM155, a novel small-molecule survivin suppressant, induces regression of established human hormone-refractory prostate tumor xenografts
    Takahito Nakahara
    Institute for Drug Discovery Research, Astellas Pharma Inc, Tsukuba shi, Ibaraki, Japan
    Cancer Res 67:8014-21. 2007
  2. ncbi Shikonin circumvents cancer drug resistance by induction of a necroptotic death
    Weidong Han
    Cancer Institute, The Second Affiliated Hospital, Zhejiang University School of Medicine, 88 Jiefang Road, Hangzhou, Zhejiang, China
    Mol Cancer Ther 6:1641-9. 2007
  3. doi A multi-center phase II evaluation of the small molecule survivin suppressor YM155 in patients with unresectable stage III or IV melanoma
    Karl D Lewis
    University of Colorado Health Sciences Center, Aurora, CO, USA
    Invest New Drugs 29:161-6. 2011
  4. ncbi Plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone) induces apoptosis and cell cycle arrest in A549 cells through p53 accumulation via c-Jun NH2-terminal kinase-mediated phosphorylation at serine 15 in vitro and in vivo
    Ya Ling Hsu
    Department of Biotechnology, Chia Nan University of Pharmacy and Science, Tainan, Taiwan
    J Pharmacol Exp Ther 318:484-94. 2006
  5. ncbi The effects on Trypanosoma cruzi of novel synthetic naphthoquinones are mediated by mitochondrial dysfunction
    Rubem F S Menna-Barreto
    Laboratorio de Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ 21040 900, Brazil
    Free Radic Biol Med 47:644-53. 2009
  6. doi YM155, a novel survivin suppressant, enhances taxane-induced apoptosis and tumor regression in a human Calu 6 lung cancer xenograft model
    Takahito Nakahara
    Institute for Drug Discovery Research, Astellas Pharma Inc, Tsukuba shi, Ibaraki, Japan
    Anticancer Drugs 22:454-62. 2011
  7. pmc An NQO1- and PARP-1-mediated cell death pathway induced in non-small-cell lung cancer cells by beta-lapachone
    Erik A Bey
    Department of Pharmacology, Laboratory of Molecular Stress Responses, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA
    Proc Natl Acad Sci U S A 104:11832-7. 2007
  8. doi Antitumor effects of YM155, a novel survivin suppressant, against human aggressive non-Hodgkin lymphoma
    Aya Kita
    Drug Discovery Research, Astellas Pharma Inc, Tsukuba shi, Ibaraki, Japan
    Leuk Res 35:787-92. 2011
  9. doi Phase I study of YM155, a novel survivin suppressant, in patients with advanced solid tumors
    Taroh Satoh
    Department of Medical Oncology, Kinki University School of Medicine, Osaka, Japan
    Clin Cancer Res 15:3872-80. 2009
  10. doi Broad spectrum and potent antitumor activities of YM155, a novel small-molecule survivin suppressant, in a wide variety of human cancer cell lines and xenograft models
    Takahito Nakahara
    Institute for Drug Discovery Research, Astellas Pharma, Inc, Tsukuba, Ibaraki, Japan
    Cancer Sci 102:614-21. 2011

Research Grants

  1. Novel Mechanisms of Quinone Toxicity
    David Ross; Fiscal Year: 2010
  2. LUNG INJURY BY NAPHTHALENES
    Alan Buckpitt; Fiscal Year: 1993
  3. LUNG INJURY BY NAPHTHALENES
    Alan Buckpitt; Fiscal Year: 1992
  4. STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF DHAQ ANALOGS
    CHIA CHUNG CHENG; Fiscal Year: 1980
  5. AZULOQUINONES: POTENTIAL NEW ANTITUMOR AGENTS
    LAWRENCE SCOTT; Fiscal Year: 1980
  6. PLANT TUMOR INHIBITORS
    David Kingston; Fiscal Year: 1980
  7. MECHANISM OF ACTION OF ANTITUMOR DRUGS
    Leroy Liu; Fiscal Year: 1993
  8. TOTAL SYNTHESIS OF THIOSTREPTON
    K Nicolaou; Fiscal Year: 2003
  9. TOTAL SYNTHESIS OF THIOSTREPTON
    K Nicolaou; Fiscal Year: 2002
  10. SYNTHESIS OF ANTIBIOTICS
    K Nicolaou; Fiscal Year: 2006

Detail Information

Publications263 found, 100 shown here

  1. ncbi YM155, a novel small-molecule survivin suppressant, induces regression of established human hormone-refractory prostate tumor xenografts
    Takahito Nakahara
    Institute for Drug Discovery Research, Astellas Pharma Inc, Tsukuba shi, Ibaraki, Japan
    Cancer Res 67:8014-21. 2007
    ..Further extensive investigation of YM155 in many types of cancer, including HRPC, seems to be worthwhile to develop this novel therapeutic approach...
  2. ncbi Shikonin circumvents cancer drug resistance by induction of a necroptotic death
    Weidong Han
    Cancer Institute, The Second Affiliated Hospital, Zhejiang University School of Medicine, 88 Jiefang Road, Hangzhou, Zhejiang, China
    Mol Cancer Ther 6:1641-9. 2007
    ..To our best knowledge, this is the first report to document the induction of necroptosis by a small molecular compound to circumvent cancer drug resistance...
  3. doi A multi-center phase II evaluation of the small molecule survivin suppressor YM155 in patients with unresectable stage III or IV melanoma
    Karl D Lewis
    University of Colorado Health Sciences Center, Aurora, CO, USA
    Invest New Drugs 29:161-6. 2011
    ..YM155 is a small molecule suppressant of survivin that has been shown in preclinical cell lines, xenograft models and phase I studies to have anti-tumor activity...
  4. ncbi Plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone) induces apoptosis and cell cycle arrest in A549 cells through p53 accumulation via c-Jun NH2-terminal kinase-mediated phosphorylation at serine 15 in vitro and in vivo
    Ya Ling Hsu
    Department of Biotechnology, Chia Nan University of Pharmacy and Science, Tainan, Taiwan
    J Pharmacol Exp Ther 318:484-94. 2006
    ..Taken together, these results suggest a critical role for JNK and p53 in plumbagin-induced G2/M arrest and apoptosis of human nonsmall cell lung cancer cells...
  5. ncbi The effects on Trypanosoma cruzi of novel synthetic naphthoquinones are mediated by mitochondrial dysfunction
    Rubem F S Menna-Barreto
    Laboratorio de Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ 21040 900, Brazil
    Free Radic Biol Med 47:644-53. 2009
    ..Our results indicate that the trypanocidal action of the naphthofuranquinones is associated with mitochondrial dysfunction, leading to increased reactive oxygen species generation and parasite death...
  6. doi YM155, a novel survivin suppressant, enhances taxane-induced apoptosis and tumor regression in a human Calu 6 lung cancer xenograft model
    Takahito Nakahara
    Institute for Drug Discovery Research, Astellas Pharma Inc, Tsukuba shi, Ibaraki, Japan
    Anticancer Drugs 22:454-62. 2011
    ....
  7. pmc An NQO1- and PARP-1-mediated cell death pathway induced in non-small-cell lung cancer cells by beta-lapachone
    Erik A Bey
    Department of Pharmacology, Laboratory of Molecular Stress Responses, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA
    Proc Natl Acad Sci U S A 104:11832-7. 2007
    ..beta-Lapachone killed cells in a tumorselective manner and is indicated for use against NQO1+ NSCLC cancers...
  8. doi Antitumor effects of YM155, a novel survivin suppressant, against human aggressive non-Hodgkin lymphoma
    Aya Kita
    Drug Discovery Research, Astellas Pharma Inc, Tsukuba shi, Ibaraki, Japan
    Leuk Res 35:787-92. 2011
    ..YM155 increased survival significantly versus rituximab in disseminated Ramos models. This study suggests that YM155 may represent an effective treatment for aggressive lymphomas...
  9. doi Phase I study of YM155, a novel survivin suppressant, in patients with advanced solid tumors
    Taroh Satoh
    Department of Medical Oncology, Kinki University School of Medicine, Osaka, Japan
    Clin Cancer Res 15:3872-80. 2009
    ..The aim of this study was to determine the maximum tolerated dose (MTD) and to assess the safety, pharmacokinetics, and antitumor activity of YM155 in patients with advanced refractory solid tumors...
  10. doi Broad spectrum and potent antitumor activities of YM155, a novel small-molecule survivin suppressant, in a wide variety of human cancer cell lines and xenograft models
    Takahito Nakahara
    Institute for Drug Discovery Research, Astellas Pharma, Inc, Tsukuba, Ibaraki, Japan
    Cancer Sci 102:614-21. 2011
    ..The broad and potent antitumor activity presented in the present study is indicative of the therapeutic potential of YM155 in the clinical setting...
  11. doi Anti-inflammatory effects of plumbagin are mediated by inhibition of NF-kappaB activation in lymphocytes
    Rahul Checker
    Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Mumbai 400085, India
    Int Immunopharmacol 9:949-58. 2009
    ..Further, plumbagin prevented Graft Versus Host Disease-induced mortality in mice. To our knowledge this is the first report showing the immunomodulatory effects of plumbagin in lymphocytes via modulation of NF-kappaB activation...
  12. ncbi Cellular pharmacology studies of shikonin derivatives
    Xin Chen
    Laboratory of Molecular Immunoregulation, Division of Basic Sciences, National Cancer Institute Frederick, MD 21702 1201, USA
    Phytother Res 16:199-209. 2002
    ..This general inhibitory effect can account for the broad spectrum of shikonin biological and pharmacological activities...
  13. doi Multicenter phase II trial of YM155, a small-molecule suppressor of survivin, in patients with advanced, refractory, non-small-cell lung cancer
    Giuseppe Giaccone
    Vrije Universiteit Medical Center, Amsterdam, The Netherlands
    J Clin Oncol 27:4481-6. 2009
    ..To evaluate the antitumor activity and safety of YM155, a novel, small-molecule suppressor of survivin, as single-agent therapy in patients with previously treated, advanced non-small-cell lung cancer (NSCLC)...
  14. doi Phase I and pharmacokinetic study of YM155, a small-molecule inhibitor of survivin
    Anthony W Tolcher
    Institute for Drug Development, Cancer Therapy and Research Center, San Antonio, TX, USA
    J Clin Oncol 26:5198-203. 2008
    ..To determine the maximum-tolerated dose (MTD) and assess the safety, pharmacokinetics, and preliminary evidence of antitumor activity of YM155, a small-molecule inhibitor of survivin...
  15. pmc Shikonin exerts antitumor activity via proteasome inhibition and cell death induction in vitro and in vivo
    Huanjie Yang
    Department of Pathophysiology, Guangzhou Medical College, Guangzhou, Guangdong, People s Republic of China
    Int J Cancer 124:2450-9. 2009
    ..Our results indicate that the tumor proteasome is one of the cellular targets of shikonin and inhibition of the proteasome activity by shikonin contributes to its antitumor property...
  16. pmc Increased age reduces DAF-16 and SKN-1 signaling and the hormetic response of Caenorhabditis elegans to the xenobiotic juglone
    Aaron J Przybysz
    Department of Pharmacology, Vanderbilt University, 1161 21st Avenue South, Nashville, TN 37232, USA
    Mech Ageing Dev 130:357-69. 2009
    ..Our studies provide a foundation for developing a molecular understanding of how age affects cytoprotective transcriptional pathways...
  17. pmc Shikonin extracted from medicinal Chinese herbs exerts anti-inflammatory effect via proteasome inhibition
    Li Lu
    Protein Modification and Degradation Lab, Department of Pathophysiology, Guangzhou Medical College, Guangzhou, Guangdong, PR China
    Eur J Pharmacol 658:242-7. 2011
    ..The novel finding about macrophage proteasome as a target of shikonin suggests that this medicinal compound has great potential to be developed into an anti-inflammatory agent...
  18. pmc Artemisinin-naphthoquine combination (ARCO) therapy for uncomplicated falciparum malaria in adults of Papua New Guinea: a preliminary report on safety and efficacy
    Francis W Hombhanje
    Faculty of Health Sciences, Divine Word University, Madang Province, Papua New Guinea
    Malar J 8:196. 2009
    ..A study was undertaken to assess the safety, efficacy and tolerability of ANQ combination in areas of multi-drug resistance to generate preliminary baseline data in adult population of Papua New Guinea...
  19. doi Shikonin, a Chinese plant-derived naphthoquinone, induces apoptosis in hepatocellular carcinoma cells through reactive oxygen species: A potential new treatment for hepatocellular carcinoma
    Ke Gong
    College of Life Sciences, Wuhan University, Wuhan 430072, People s Republic of China
    Free Radic Biol Med 51:2259-71. 2011
    ..Taken together, our data show that shikonin, which may be a promising agent in the treatment of liver cancer, induced apoptosis in HCC cells through the ROS/Akt and RIP1/NF-κB pathways...
  20. ncbi A shikonin derivative, beta-hydroxyisovalerylshikonin, is an ATP-non-competitive inhibitor of protein tyrosine kinases
    Kazuyasu Nakaya
    School of Pharmaceutical Sciences, Showa University, Tokyo, Japan
    Anticancer Drugs 14:683-93. 2003
    ....
  21. ncbi Multiple stressors in Caenorhabditis elegans induce stress hormesis and extended longevity
    James R Cypser
    Institute for Behavioral Genetics, University of Colorado, Boulder 80303, USA
    J Gerontol A Biol Sci Med Sci 57:B109-14. 2002
    ..In dose-response studies, induced thermotolerance paralleled the induced increase in life expectancy, which is consistent with a common origin...
  22. pmc Prostate cancer radiosensitization through poly(ADP-Ribose) polymerase-1 hyperactivation
    Ying Dong
    Departments of Pharmacology, Radiation Oncology, Pathology, Biostatistics and Clinical Sciences, and Urology, Simmons Comprehensive Cancer Center, University of Texas Southwestern Medical Center, Dallas, TX 75390 8807, USA
    Cancer Res 70:8088-96. 2010
    ..Our findings offer a rationale for the clinical utilization of β-lap (Arq 501) as a radiosensitizer in prostate cancers that overexpress NQO1, offering a potentially synergistic targeting strategy to exploit PARP-1 hyperactivation...
  23. doi Plumbagin-induced apoptosis of human breast cancer cells is mediated by inactivation of NF-kappaB and Bcl-2
    Aamir Ahmad
    Department of Pathology, Barbara Ann Karmanos Cancer Center and Wayne State University School of Medicine, Detroit, Michigan 48201, USA
    J Cell Biochem 105:1461-71. 2008
    ....
  24. ncbi Selective induction of necrotic cell death in cancer cells by beta-lapachone through activation of DNA damage response pathway
    Xiangao Sun
    Department of Therapeutic Biology, ArQule Biomedical Institute, Norwood, Massachusetts 02062, USA
    Cell Cycle 5:2029-35. 2006
    ..Our data suggest that selective necrotic cell death can be induced through activation of DNA damage response pathways, supporting the idea of selective necrotic cell death as a therapeutic strategy to eliminate cancer cells...
  25. ncbi Alkannins and shikonins: a new class of wound healing agents
    V P Papageorgiou
    Laboratory of Organic Chemistry, Department of Chemical Engineering, Aristotle University of Thessaloniki, Greece
    Curr Med Chem 15:3248-67. 2008
    ..In this paper we review the findings and advances on the molecular and biological properties of A/S that promote wound healing...
  26. doi The trypanocidal activity of naphthoquinones: a review
    Antonio Ventura Pinto
    Núcleo de Pesquisas em Produtos Naturais, Centro de Ciencias da Saude, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil
    Molecules 14:4570-90. 2009
    b>Naphthoquinones are compounds present in several families of higher plants. Their molecular structures confer redox properties, and they are involved in multiple biological oxidative processes...
  27. ncbi Calcium is a key signaling molecule in beta-lapachone-mediated cell death
    C Tagliarino
    Departments of Radiation Oncology and Pharmacology, Department of Anatomy, Case Western Reserve University, Cleveland, Ohio 44106-4942, USA
    J Biol Chem 276:19150-9. 2001
    ..Use of beta-Lap to trigger an apparently novel, calpain-like-mediated apoptotic cell death could be useful for breast and prostate cancer therapy...
  28. pmc Pharmacological stimulation of NADH oxidation ameliorates obesity and related phenotypes in mice
    Jung Hwan Hwang
    Department of Internal Medicine, Chungnam National University School of Medicine, Daejeon, Korea
    Diabetes 58:965-74. 2009
    ..We tried to determine whether pharmacological stimulation of NADH oxidation provides therapeutic effects in rodent models of metabolic syndrome...
  29. doi Necrostatin-1 reverts shikonin-induced necroptosis to apoptosis
    Weidong Han
    Cancer Institute, The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang, 310009, China
    Apoptosis 14:674-86. 2009
    ..To the best of our knowledge, this is the first study to document a conversion from necroptosis to apoptosis...
  30. ncbi Cytochrome b mutations that modify the ubiquinol-binding pocket of the cytochrome bc1 complex and confer anti-malarial drug resistance in Saccharomyces cerevisiae
    Jacques J Kessl
    Department of Biochemistry, Dartmouth Medical School, Hanover, New Hampshire 03755
    J Biol Chem 280:17142-8. 2005
    ..By modeling the variations in cytochrome b structure and atovaquone binding with the mutated bc1 complexes, we obtained the first quantitative explanation for the molecular basis of atovaquone resistance in malaria parasites...
  31. ncbi Natural products as antiparasitic drugs
    O Kayser
    Freie Universitat Berlin, Institut fur Pharmazie, Pharmazeutische Biotechnologie, Kelchstrasse 31, 12169 Berlin, Germany
    Parasitol Res 90:S55-62. 2003
    ..Many novel lead structures, however, have severe chemico-physical drawbacks such as poor solubility. Here, innovative drug formulations and carrier systems might help, as discussed by the authors in another article of this series...
  32. doi Caenorhabditis elegans lifespan extension caused by treatment with an orally active ROS-generator is dependent on DAF-16 and SIR-2.1
    Tanja Heidler
    Department of Food and Nutrition, Molecular Nutrition Unit, Technical University of Munich, Am Forum 5, Freising, Germany
    Biogerontology 11:183-95. 2010
    ..1-dependent alterations in gene expression after a ROS challenge lead to a lifespan extension in C. elegans as long as the stressor concentration does not exceed the saturable protective capacity...
  33. ncbi p53-mediated cell cycle arrest and apoptosis induced by shikonin via a caspase-9-dependent mechanism in human malignant melanoma A375-S2 cells
    Zhen Wu
    Department of Phytochemistry, Shenyang Pharmaceutical University, P R China
    J Pharmacol Sci 94:166-76. 2004
    ..Apoptosis-inducing factor, another apoptotic protein of mitochondria, partially contributed to shikonin-induced release of cytochrome c. Taken together, shikonin-induced DNA damage activates p53 and caspase-9 pathways...
  34. doi Naturally-occurring shikonin analogues--a class of necroptotic inducers that circumvent cancer drug resistance
    Yanyan Xuan
    Cancer Institute, The Key Laboratory of Cancer Prevention and Intervention, China National Ministry of Education, The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang 310009, China
    Cancer Lett 274:233-42. 2009
    ..The results strengthen the previous findings that necroptotic induction could circumvent a broad spectrum of cancer drug resistance...
  35. ncbi Calcium-dependent modulation of poly(ADP-ribose) polymerase-1 alters cellular metabolism and DNA repair
    Melissa S Bentle
    Department of Pharmacology, Case Western Reserve University, Cleveland, Ohio 44106, USA
    J Biol Chem 281:33684-96. 2006
    ..Thus, Ca(2+) appears to be an important co-factor in PARP-1 hyperactivation after ROS-induced DNA damage, which alters cellular metabolism and DNA repair...
  36. pmc Selective killing of cancer cells by beta -lapachone: direct checkpoint activation as a strategy against cancer
    Youzhi Li
    Division of Gastroenterology, Beth Israel Deaconess Medical Center, Harvard Medical School, 330 Brookline Avenue, Boston, MA 02215, USA
    Proc Natl Acad Sci U S A 100:2674-8. 2003
    ..This study suggests direct checkpoint activation as a strategy against cancer...
  37. ncbi Plumbagin induces cell cycle arrest and apoptosis through reactive oxygen species/c-Jun N-terminal kinase pathways in human melanoma A375.S2 cells
    Clay C C Wang
    Department of Chemistry, University of Southern California, College of Letters, Arts, and Sciences, University Park Campus, Los Angeles, CA 90089, USA
    Cancer Lett 259:82-98. 2008
    ..Moreover, blocking ERK and JNK by specific inhibitors suppressed plumbagin-triggered mitochondrial apoptotic pathway. Taken together, these results imply a critical role for ROS and JNK in the plumbagin's anticancer activity...
  38. ncbi The biosynthetic pathway for aurofusarin in Fusarium graminearum reveals a close link between the naphthoquinones and naphthopyrones
    Rasmus J N Frandsen
    Department of Ecology, The Royal Veterinary and Agricultural University, DK 1871 Frederiksberg C, Copenhagen, Denmark
    Mol Microbiol 61:1069-80. 2006
    ..This links the biosynthesis of naphthopyrones and naphthoquinones together...
  39. pmc Differential functional genomic effects of anti-inflammatory phytocompounds on immune signaling
    Shao Chih Chiu
    Graduate Institute of Immunology, China Medical University, 91 Hsueh Shih Rd, Taichung 40402, Taiwan
    BMC Genomics 11:513. 2010
    ....
  40. doi Design, synthesis and biological evaluation of novel nitrogen and sulfur containing hetero-1,4-naphthoquinones as potent antifungal and antibacterial agents
    Vishnu K Tandon
    Department of Chemistry, University of Lucknow, Lucknow, India
    Eur J Med Chem 44:3130-7. 2009
    A series of 2-Arylamino-3-chloro-1,4-naphthoquinones (3), 2-Amino-3-arylsulfanyl-1,4-naphthoquinones (5), 2-Arylamino-3-arylsulfanyl-1,4-naphthoquinones (6), Dihydrobenzo[f]naphtho[2,3-b][1,4]thiazepine-6,11-diones (9) (via Pictet-..
  41. ncbi Induction of apoptosis by shikonin through a ROS/JNK-mediated process in Bcr/Abl-positive chronic myelogenous leukemia (CML) cells
    Xin Mao
    1State Key Laboratory of Virology, College of Life Sciences, Wuhan University, Wuhan 430072, China
    Cell Res 18:879-88. 2008
    ..Our data also suggest that shikonin may be a promising agent for the treatment of CML, as a generator of ROS...
  42. ncbi Antimicrobial activities of naphthazarins from Arnebia euchroma
    Chien Chang Shen
    National Research Institute of Chinese Medicine, Taipei 112, Taiwan
    J Nat Prod 65:1857-62. 2002
    ..6-5.4 microg/mL (CD(50)). Our results indicate that the ester derivatives of alkannin are potential candidates of anti-MRSA and anti-VRE agents with antitumor activity...
  43. ncbi Plumbagin induces cell death through a copper-redox cycle mechanism in human cancer cells
    S Nazeem
    Department of Biochemistry, Faculty of Life Sciences, Aligarh Muslim University, Aligarh 202002, Uttar Pradesh, India
    Mutagenesis 24:413-8. 2009
    ....
  44. ncbi Causal prophylactic efficacy of atovaquone-proguanil (Malarone) in a human challenge model
    J D Berman
    Walter Reed Army Institute of Research, Silver Spring, MD 20910, USA
    Trans R Soc Trop Med Hyg 95:429-32. 2001
    ..No atovaquone-proguanil volunteer acquired malaria. Atovaquone-proguanil is the first licensed antimalarial agent that kills P. falciparum in the liver and that may be discontinued 7 days after the last exposure...
  45. doi Efficacy of oral single dose therapy with artemisinin-naphthoquine phosphate in uncomplicated falciparum malaria
    Thein Tun
    Department of Medical Research Upper Myanmar, Anisakhan, Pyin Oo Lwin 05062, Mandalay Division, Myanmar
    Acta Trop 111:275-8. 2009
    ..The drug was well tolerated and no adverse reactions were detected in the patients. Since it is a single dose therapy, health workers can administer the drug as directly observed treatment...
  46. ncbi In vitro antifungal activity of naphthoquinone derivatives
    Kenroh Sasaki
    Tohoku Pharmaceutical University, Sendai, Japan
    Biol Pharm Bull 25:669-70. 2002
    ..krusei compared with the standard. Against the filamentous fungus, Trichosporon cutaneum, all naphthoquinones were found to have a range of activity with lower potency than standard...
  47. doi Initial response and cellular protection through the Keap1/Nrf2 system during the exposure of primary mouse hepatocytes to 1,2-naphthoquinone
    Takashi Miura
    Doctoral Programs in Medical Sciences, Graduate School of Comprehensive Human Sciences, Graduate School of Life and Environmental Sciences, University of Tsukuba, 1 1 1 Tennodai, Tsukuba, Ibaraki, Japan
    Chem Res Toxicol 24:559-67. 2011
    ..These findings suggest that the Keap1/Nrf2 system is essential for the prevention of cell damage resulting from exposure to 1,2-NQ...
  48. ncbi Atovaquone-proguanil versus mefloquine for malaria prophylaxis in nonimmune travelers: results from a randomized, double-blind study
    D Overbosch
    Harbor Hospital and Institute of Tropical Medicine, Rotterdam, The Netherlands
    Clin Infect Dis 33:1015-21. 2001
    ..No confirmed diagnoses of malaria occurred in either group. Atovaquone-proguanil was better tolerated than was mefloquine, and it was similarly effective for malaria prophylaxis in nonimmune travelers...
  49. doi Shikonin derivatives inhibited LPS-induced NOS in RAW 264.7 cells via downregulation of MAPK/NF-kappaB signaling
    Yu Wen Cheng
    School of Pharmacy, Taipei Medical University, Taipei, Taiwan, Republic of China
    J Ethnopharmacol 120:264-71. 2008
    ..In the present study, the effect and the underline molecular mechanism of shikonin derivatives isolated from root extracts of Lithospermum euchroma on lipopolysaccharide (LPS)-induced inflammatory response were investigated...
  50. ncbi Natural and synthetic naphthoquinones active against Trypanosoma cruzi: an initial step towards new drugs for Chagas disease
    Cristian O Salas
    Facultad de Quimica, Pontificia Universidad Catolica de Chile, Casilla 306, Santiago 6094411, Chile
    Curr Med Chem 18:144-61. 2011
    ..An overview of a number of natural naphthoquinones tested against T. cruzi parasites is provided...
  51. ncbi Plumbagin induces G2-M arrest and autophagy by inhibiting the AKT/mammalian target of rapamycin pathway in breast cancer cells
    Po Lin Kuo
    Cell Biology Laboratory, Department of Biotechnology, Chia Nan University of Pharmacy and Science, Tainan 717, Taiwan
    Mol Cancer Ther 5:3209-21. 2006
    ..Taken together, these results imply a critical role for AKT inhibition in plumbagin-induced G2-M arrest and autophagy of human breast cancer cells...
  52. doi Design of anti-parasitic and anti-fungal hydroxy-naphthoquinones that are less susceptible to drug resistance
    Louise M Hughes
    Department of Biochemistry, Dartmouth Medical School, 7200 Vail, Hanover, NH 03755, USA
    Mol Biochem Parasitol 177:12-9. 2011
    ..fungi and overcome drug resistance, we have synthesized and tested the inhibitory activity of novel hydroxy-naphthoquinones against blood stage P. falciparum and liver stage P...
  53. ncbi Novel multiple apoptotic mechanism of shikonin in human glioma cells
    Ching Hsein Chen
    Department of Microbiology, Immunology and Biopharmaceuticals, College of Life Sciences, National Chiayi University, Chiayi, Taiwan, ROC
    Ann Surg Oncol 19:3097-106. 2012
    ..However, the anticancer mechanism of shikonin in human glioma cells is unclear at present. In the present study, we demonstrated that shikonin induces apoptosis in three human glioma cell lines: U87MG, Hs683, and M059K cells...
  54. pmc Plumbagin inhibits proliferative and inflammatory responses of T cells independent of ROS generation but by modulating intracellular thiols
    Rahul Checker
    Radiation Biology and Health Sciences Division, Bio Medical Group, Bhabha Atomic Research Centre, Mumbai 400085, Maharashtra, India
    J Cell Biochem 110:1082-93. 2010
    ..Our results for the first time show that antiproliferative effects of plumbagin are mediated by modulation of cellular redox. These results provide a rationale for application of thiol-depleting agents as anti-inflammatory drugs...
  55. doi Chemical inducers of heat shock proteins derived from medicinal plants and cytoprotective genes response
    Kanwal Ahmed
    Division of Gastrointestinal Pathophysiology, Institute of Natural Medicine, University of Toyama, Toyama, Japan
    Int J Hyperthermia 28:1-8. 2012
    ..In short, the detailed mechanisms of Hsp70 induction by shikonin is not fully understood, Nrf2 and its target genes might be involved in the Hsp70 up-regulation in U937 cells...
  56. pmc Tabebuia avellanedae naphthoquinones: activity against methicillin-resistant staphylococcal strains, cytotoxic activity and in vivo dermal irritability analysis
    Eliezer Menezes Pereira
    Instituto de Microbiologia Prof, Paulo de Góes, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil
    Ann Clin Microbiol Antimicrob 5:5. 2006
    ..In addition, its mechanism of action was also analyzed...
  57. pmc Marked anti-tumour activity of the combination of YM155, a novel survivin suppressant, and platinum-based drugs
    T Iwasa
    Department of Medical Oncology, Kinki University School of Medicine, 377 2 Ohno Higashi, Osaka Sayama, Osaka 589 8511, Japan
    Br J Cancer 103:36-42. 2010
    ..We have now investigated the effects of the combination of YM155, a novel small-molecule inhibitor of survivin expression, and platinum compounds (cisplatin and carboplatin) on human non-small cell lung cancer (NSCLC) cell lines...
  58. ncbi Activity of 7-methyljuglone derivatives against Mycobacterium tuberculosis and as subversive substrates for mycothiol disulfide reductase
    Anita Mahapatra
    Department of Botany, Faculty of Natural and Agricultural Sciences, University of Pretoria, Pretoria 0002, South Africa
    Bioorg Med Chem 15:7638-46. 2007
    ..g. other disulfide reductases)...
  59. doi Targeted BIRC5 silencing using YM155 causes cell death in neuroblastoma cells with low ABCB1 expression
    Fieke Lamers
    Department of Oncogenomics, Academic Medical Center, University of Amsterdam, Meibergdreef 15, PO Box 22700, 1105 AZ Amsterdam, The Netherlands
    Eur J Cancer 48:763-71. 2012
    ..Therefore YM155 is a promising novel compound for treatment of neuroblastoma with low ABCB1 expression...
  60. doi Studies on terpenoids produced by actinomycetes. 5-dimethylallylindole-3-carboxylic Acid and A80915G-8"-acid produced by marine-derived Streptomyces sp. MS239
    Keiichiro Motohashi
    Faculty of Applied Biosciences, Tokyo University of Agriculture, Sakuragaoka, Setagaya Ku, Tokyo, Japan
    J Antibiot (Tokyo) 61:75-80. 2008
    ..MS239, two new terpenoids named 5-dimethylallylindole-3-carboxylic acid and A80915G-8''-acid were isolated and their structures were determined mainly by NMR analyses...
  61. doi Topoisomerase inhibitors as anti-arthritic agents
    J K Jackson
    Faculty of Pharmaceutical Sciences, University of British Columbia, Vancouver, B C, V6T 1Z3, Canada
    Inflamm Res 57:126-34. 2008
    ..The objective of this study was to investigate a variety of structurally unrelated anticancer topoisomerase inhibiting agents as inhibitors of aspects of these disease processes involved in RA...
  62. ncbi Autoxidation of naphthohydroquinones: effects of pH, naphthoquinones and superoxide dismutase
    R Munday
    AgResearch, Ruakura Agricultural Research Centre, Hamilton, New Zealand
    Free Radic Res 32:245-53. 2000
    ..This may be due to differences in the rate or mechanism of autoxidation of the hydroquinones that are formed, and the data gained in this study will provide a framework for testing this possibility...
  63. doi Genotoxicity of plumbagin and its effects on catechol and NQNO-induced DNA damage in mouse lymphoma cells
    Jemal Demma
    Department of Pharmaceutical Biosciences, Uppsala University, Division of Toxicology, Box 594, BMC, SE 751 24 Uppsala, Sweden
    Toxicol In Vitro 23:266-71. 2009
    ..The fact that non-DNA damaging concentrations of plumbagin diminished the DNA damage induced by catechol, provides further support for the idea that plumbagin may act as an antioxidative agent at low concentrations...
  64. ncbi Shikonins, phytocompounds from Lithospermum erythrorhizon, inhibit the transcriptional activation of human tumor necrosis factor alpha promoter in vivo
    Vanisree Staniforth
    Institute of BioAgricultural Sciences, Academia Sinica, Taipei 11529, Taiwan, Republic of China
    J Biol Chem 279:5877-85. 2004
    ..Thus, shikonins may have clinical potential as anti-inflammatory therapeutics...
  65. doi Effect of hydroxy substituent on the prooxidant action of naphthoquinone compounds
    Keiko Murakami
    Department of Biochemistry, Aichi Medical University School of Medicine, Nagakute, Aichi 480 1195, Japan
    Toxicol In Vitro 24:905-9. 2010
    ..b>Naphthoquinones with electron-repelling hydroxyl group in the benzene moiety such as juglone and shikonin of lower ..
  66. ncbi Growth inhibition and induction of apoptosis in human oral squamous cell carcinoma Tca-8113 cell lines by Shikonin was partly through the inactivation of NF-kappaB pathway
    Ruan Min
    Department of Oral and Maxillofacial Surgery, Affiliated No 9 People s Hospital, College of Medicine, Shanghai Jiao Tong University, Shanghai 200011, PRC
    Phytother Res 22:407-15. 2008
    ..Pharmacological inhibition of the NF-kappaB activity by Shikonin might be a powerful treatment option for OSCC in which activation of NF-kappaB plays a critical role in tumor growth and progression...
  67. ncbi Efficacy of beta-lapachone in pancreatic cancer treatment: exploiting the novel, therapeutic target NQO1
    Matthew Ough
    Department of Surgery, University of Iowa College of Medicine, Iowa City, Iowa 52242, USA
    Cancer Biol Ther 4:95-102. 2005
    ....
  68. doi Plumbagin, isolated from Plumbago zeylanica, induces cell death through apoptosis in human pancreatic cancer cells
    Chien An Chen
    Department of Radiation Oncology, Far Eastern Memorial Hospital, Graduate Institute of Traditional Chinese Medicine, Chang Gung University, Taoyuan, Taiwan
    Pancreatology 9:797-809. 2009
    ..Several studies have indicated that plumbagin isolated from Plumbago zeylanica possesses anticancer activity. However, its antitumor effects against pancreatic cancer have not been explored...
  69. pmc Naphthoquinones and anthraquinones from scent glands of a dyspnoid Harvestman, Paranemastoma quadripunctatum
    Günther Raspotnig
    Institute of Zoology, Karl Franzens University, and University Children s Hospital, Universitatsplatz 2, 8010, Graz, Austria
    J Chem Ecol 36:158-62. 2010
    ..The minor components were 1,4-naphthalenediol, two methoxy-naphthoquinones (2-methoxy-1,4-naphthoquinone, and 2-methoxy-6-methyl-1,4-naphthoquinone) and two anthraquinones (2-methyl-9,..
  70. ncbi Radiosensitizing effects of plumbagin in cervical cancer cells is through modulation of apoptotic pathway
    Sreekala Nair
    Translational Cancer Research Laboratory, Rajiv Gandhi Center for Biotechnology, Thiruvananthapuram, India
    Mol Carcinog 47:22-33. 2008
    ....
  71. pmc Superoxide protects Escherichia coli from bleomycin mediated lethality
    Richard M Burger
    Public Health Research Institute, New Jersey Medical School, UMDNJ, Newark, 07103, USA
    J Inorg Biochem 103:1273-7. 2009
    ..Thus, superoxide interferes with bleomycin cytotoxicity in ways not readily explained by genetic pathways expected to protect from oxidative damage...
  72. ncbi Inhibition of tumor necrosis factor-alpha through selective blockade of Pre-mRNA splicing by shikonin
    Shao Chih Chiu
    Graduate Institute of Life Sciences, National Defense Medical Center and Agricultural Biotechnology Research Center, Academia Sinica, Taipei, Taiwan, ROC
    Mol Pharmacol 71:1640-5. 2007
    ....
  73. ncbi Plumbagin induces ROS-mediated apoptosis in human promyelocytic leukemia cells in vivo
    Kai Hong Xu
    Peking University People s Hospital, Institute of Hematology, Beijing, China
    Leuk Res 34:658-65. 2010
    ..These results indicate that plumbagin has potential as a novel therapeutic agent for myeloid leukemia...
  74. ncbi Comparison of the cytotoxic activities of naturally occurring hydroxyanthraquinones and hydroxynaphthoquinones
    Xing Ri Cui
    Faculty of Pharmaceutical Sciences, Josai University, Keyakidai 1 1, Sakado, Saitama 350 0295, Japan
    Eur J Med Chem 43:1206-15. 2008
    ..22+/-0.03 to 0.59+/-0.06 microM in the case of Hep G2 cells) as well as shikonin 10 (IC(50) values: 0.32+/-0.02 microM in the case of HCT 116 cells and 0.24+/-0.03 microM in the case of Hep G2 cells)...
  75. doi Shikonin inhibits fat accumulation in 3T3-L1 adipocytes
    Haeyong Lee
    Department of Microbiology, College of Medicine, Chung Ang University, Seoul 156 756, Korea
    Phytother Res 24:344-51. 2010
    ..Together, these changes result in the down-regulation of lipid metabolizing enzymes and reduced fat accumulation...
  76. ncbi Susceptibility of cancer cells to beta-lapachone is enhanced by ionizing radiation
    Heon Joo Park
    Radiobiology Laboratory, Department of Therapeutic Radiology, University of Minnesota Medical School, Minneapolis, MN 55455, USA
    Int J Radiat Oncol Biol Phys 61:212-9. 2005
    ..To reveal the interaction between beta-lapachone (beta-lap) and ionizing radiation (IR) in causing clonogenic death in cancer cells and to elucidate the potential usefulness of beta-lap treatment in combination with radiotherapy of cancer...
  77. ncbi Antioxidant properties of Plumbago zeylanica, an Indian medicinal plant and its active ingredient, plumbagin
    Jai C Tilak
    Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Mumbai, India
    Redox Rep 9:219-27. 2004
    ..8 x 10(8) dm(3)mol(-1)s(-1). In conclusion, our studies reveal that extracts of P. zeylanica and its active ingredient plumbagin have significant antioxidant abilities that may possibly explain some of the reported therapeutic effects...
  78. ncbi Plumbagin induces reactive oxygen species, which mediate apoptosis in human cervical cancer cells
    Priya Srinivas
    Division of Cancer Biology, Rajiv Gandhi Centre for Biotechnology, Thiruvananthapuram, Kerala, India
    Mol Carcinog 40:201-11. 2004
    ....
  79. ncbi Induction of apoptosis by shikonin through coordinative modulation of the Bcl-2 family, p27, and p53, release of cytochrome c, and sequential activation of caspases in human colorectal carcinoma cells
    Ping Chi Hsu
    Department of Seafood Science, National Kaohsiung Marine University, Kaohsiung, Taiwan
    J Agric Food Chem 52:6330-7. 2004
    ..The induction of apoptosis by shikonin may provide a pivotal mechanism for its cancer chemopreventive action...
  80. ncbi Cancer therapy with beta-lapachone
    Arthur B Pardee
    Dana Farber Cancer Institute, 44 Binney Street, Boston, MA 02115, USA
    Curr Cancer Drug Targets 2:227-42. 2002
    ..Beta-lapachone is one of a few novel anticancer drugs currently under active investigation, and it shows promise for chemotherapy alone and especially in combinations...
  81. ncbi Antitumor activities of a newly synthesized shikonin derivative, 2-hyim-DMNQ-S-33
    S H Kim
    Department of Oncology, Graduate School of East West Medical Science, Kyunghee University, 1 Seochun ri, Kiheung eup, 449 701, Yongin, South Korea
    Cancer Lett 172:171-5. 2001
    ..These findings indicate that 2-hyim-DMSQ-S33 exerts antitumor activities by regulating pERK, JNK and PKC-alpha...
  82. ncbi Molecular basis for atovaquone binding to the cytochrome bc1 complex
    Jacques J Kessl
    Department of Biochemistry, Dartmouth Medical School, Hanover, New Hampshire 03755, USA
    J Biol Chem 278:31312-8. 2003
    ..These results provide the first molecular description of how atovaquone binds to the bc1 complex and explain the differential inhibition of the fungal versus mammalian enzymes...
  83. ncbi Involvement of endoplasmic reticulum stress and activation of MAP kinases in beta-lapachone-induced human prostate cancer cell apoptosis
    Yi Chen Lien
    Institute of Anatomy and Cell Biology, School of Medicine, National Yang Ming University, Taiwan
    Histol Histopathol 23:1299-308. 2008
    ..These findings show that beta-lapachone-induced ER stress and MAP kinase phosphorylation is a novel signaling pathway underlying the molecular mechanism of the anticancer effect of beta-lapachone...
  84. ncbi Radiosensitizing effect of YM155, a novel small-molecule survivin suppressant, in non-small cell lung cancer cell lines
    Tsutomu Iwasa
    Department of Medical Oncology, Kinki University School of Medicine, Osaka Sayama, Osaka, Japan
    Clin Cancer Res 14:6496-504. 2008
    ..We have now investigated the effect of YM155, a small-molecule inhibitor of survivin expression, on the sensitivity of human non-small cell lung cancer (NSCLC) cell lines to gamma-radiation...
  85. pmc Putative polyketide synthase and laccase genes for biosynthesis of aurofusarin in Gibberella zeae
    Jung Eun Kim
    School of Agricultural Biotechnology and Center for Agricultural Biomaterials, Seoul National University, Seoul, Korea
    Appl Environ Microbiol 71:1701-8. 2005
    ..zeae. This information is the first information concerning the biosynthesis of these pigments by G. zeae and could help in studies of their toxicity in domesticated animals...
  86. ncbi Plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone) suppresses NF-kappaB activation and NF-kappaB-regulated gene products through modulation of p65 and IkappaBalpha kinase activation, leading to potentiation of apoptosis induced by cytokine and chemotherape
    Santosh K Sandur
    Cytokine Research Laboratory, Department of Experimental Therapeutics, Unit 143, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    J Biol Chem 281:17023-33. 2006
    ..This may explain its cell growth modulatory, anticarcinogenic, and radiosensitizing effects previously described...
  87. ncbi Inhibition of Nox-4 activity by plumbagin, a plant-derived bioactive naphthoquinone
    Yaxian Ding
    Department of Medicine, Case Western Reserve University and University Hospital of Cleveland, Cleveland, Ohio 44106, USA
    J Pharm Pharmacol 57:111-6. 2005
    ..Furthermore, plumbagin inhibited the superoxide production in Nox-4 transfected COS-7 cells. These results indicated that plumbagin directly interacted with Nox-4 and inhibited its activity...
  88. ncbi Effects of naphthoquinone on airway responsiveness in the presence or absence of antigen in mice
    Ken ichiro Inoue
    Environmental Health Sciences Division, National Institute for Environmental Studies, 16 2 Onogawa, Tsukuba, Ibaraki, 305 8506, Japan
    Arch Toxicol 81:575-81. 2007
    ..These results indicate that NQ can enhance airway hyperresponsiveness in the presence or absence of an antigen. Also, amplified lung expressions of IL-13 and MUC5AC might partly contribute to the deterioration of asthma features by NQ...
  89. doi A naphthoquinone derivative can induce anemia through phosphatidylserine exposure-mediated erythrophagocytosis
    Ji Yoon Noh
    College of Pharmacy, Seoul National University, Seoul, Korea
    J Pharmacol Exp Ther 333:414-20. 2010
    ..In conclusion, these results suggest that betaL-induced anemia might be mediated through the PS exposure and subsequent erythrophagocytosis, providing novel insight into the drug-induced anemia...
  90. pmc Shikonin, a component of chinese herbal medicine, inhibits chemokine receptor function and suppresses human immunodeficiency virus type 1
    Xin Chen
    Basic Research Program, SAIC Frederick, Inc, National Cancer Institute Frederick, Frederick, Maryland 21702 1201, USA
    Antimicrob Agents Chemother 47:2810-6. 2003
    ..Therefore, shikonin, as a naturally occurring, low-molecular-weight pan-chemokine receptor inhibitor, constitutes a basis for the development of novel anti-HIV therapeutic agents...
  91. ncbi SH-7, a new synthesized shikonin derivative, exerting its potent antitumor activities as a topoisomerase inhibitor
    Fan Yang
    State Key Laboratory of Drug Research, Division of Anti tumor Pharmacology, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, People s Republic of China
    Int J Cancer 119:1184-93. 2006
    ..The well-defined Topo II inhibitory activity, antitumor effects particularly with its obvious anti-MDR action, better solubility and less toxicity make SH-7 as a potential antitumor drug candidate for further research and development...
  92. pmc Plumbagin, a medicinal plant-derived naphthoquinone, is a novel inhibitor of the growth and invasion of hormone-refractory prostate cancer
    Moammir H Aziz
    Department of Human Oncology, School of Medicine and Public Health, University of Wisconsin, Madison, Wisconsin 53792, USA
    Cancer Res 68:9024-32. 2008
    ..PL inhibits multiple molecular targets including PKCepsilon, a predictive biomarker of PCa aggressiveness. PL may be a novel agent for therapy of hormone-refractory PCa...
  93. pmc Endoplasmic reticulum stress-induced JNK activation is a critical event leading to mitochondria-mediated cell death caused by β-lapachone treatment
    Hyemi Lee
    Department of Microbiology, College of Medicine, Center for Advanced Medical Education by BK21 Project, Inha University, Incheon, Republic of Korea
    PLoS ONE 6:e21533. 2011
    ..Although β-lap has been reported to induce apoptosis in various cancer types in an NQO1-dependent manner, the signaling pathways by which β-lap causes apoptosis are poorly understood...
  94. ncbi Anticancer mechanism of plumbagin, a natural compound, on non-small cell lung cancer cells
    Rohini Gomathinayagam
    Department of Clinical Sciences, College of Health Sciences, University of Kentucky, Lexington, KY 40536 0200, USA
    Anticancer Res 28:785-92. 2008
    ..Hence, better therapeutic options are immediately required for lung cancer. Plumbagin, a natural compound has been recently examined for its anticancer effect on different cancers...
  95. ncbi Nonhomologous end joining is essential for cellular resistance to the novel antitumor agent, beta-lapachone
    Melissa S Bentle
    Department of Pharmacology, Case Western Reserve University, Cleveland, OH, USA
    Cancer Res 67:6936-45. 2007
    ....
  96. pmc Mutations in cytochrome b resulting in atovaquone resistance are associated with loss of fitness in Plasmodium falciparum
    Jennifer M Peters
    Malaria Laboratory, Infectious Diseases Unit, The Queensland Institute of Medical Research, Queensland, Australia
    Antimicrob Agents Chemother 46:2435-41. 2002
    ..Our results suggest that the prevalence of resistant parasites may decrease after the drug usage is discontinued...
  97. ncbi Plumbagin-induced apoptosis in human prostate cancer cells is associated with modulation of cellular redox status and generation of reactive oxygen species
    Anna A Powolny
    Department of Pharmacology and Urology, University of Pittsburgh Cancer Institute, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania, USA
    Pharm Res 25:2171-80. 2008
    ..To investigate the mechanism of human prostate cancer cell growth inhibition by plumbagin, a constituent of the widely used medicinal herb Plumbago zeylanica L...
  98. pmc Inhibition of lysine acetyltransferase KAT3B/p300 activity by a naturally occurring hydroxynaphthoquinone, plumbagin
    Kodihalli C Ravindra
    Transcription and Disease Laboratory, Molecular Biology and Genetics Unit, Jawaharlal Nehru Centre for Advanced Scientific Research, Jakkur, Bangalore 560064, India
    J Biol Chem 284:24453-64. 2009
    ..This study describes for the first time the chemical entity (hydroxyl group) required for the inhibition of acetyltransferase activity...
  99. pmc Cytotoxicity mechanism of two naphthoquinones (menadione and plumbagin) in Saccharomyces cerevisiae
    Frederico Augusto Vieira Castro
    Departamento de Bioquimica, Laboratório de Investigação de Fatores de Estresse, Instituto de Quimica, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brasil
    PLoS ONE 3:e3999. 2008
    ..However, due to differences in structures and diverse pharmacological effects, the exact toxicity mechanisms exerted by quinones are far from elucidatation...
  100. ncbi Chemical knockdown of protein-tyrosine phosphatase 1B by 1,2-naphthoquinone through covalent modification causes persistent transactivation of epidermal growth factor receptor
    Noriko Iwamoto
    Doctoral Programs in Medical Sciences, Graduate School of Comprehensive Human Sciences, University of Tsukuba, 1 1 1 Tennoudai, Tsukuba, Ibaraki 305 8575, Japan
    J Biol Chem 282:33396-404. 2007
    ..Collectively, the results show that covalent attachment of 1,2-NQ to PTP1B is at least partially responsible for the reduction of PTP activity, which leads to prolonged transactivation of EGFR in the cells...
  101. ncbi Antibacterial and antiviral naphthazarins from Maharanga bicolor
    M Rajbhandari
    Research Center for Applied Science and Technology, Tribhuvan University, Kathmandu, Nepal
    Pharmazie 62:633-5. 2007
    ..Compounds 2-5 showed antibacterial activity against multi resistant human pathogenic Staphylococcus and Enterococcus species and 1, 4 and 5 showed antiviral activity against herpes simplex virus type-1...

Research Grants93

  1. Novel Mechanisms of Quinone Toxicity
    David Ross; Fiscal Year: 2010
    DESCRIPTION (provided by applicant): Both benzoquinones and naphthoquinones have been found to perturb protein handling and degradation in a variety of cellular systems...
  2. LUNG INJURY BY NAPHTHALENES
    Alan Buckpitt; Fiscal Year: 1993
    ..2) S- thiolation of proteins in susceptible cells results from exposure to either naphthalene (mediated by naphthoquinones) or 2-methylnaphthalene; 3) naphthalene oxides diffusing from metabolically active cells are capable of ..
  3. LUNG INJURY BY NAPHTHALENES
    Alan Buckpitt; Fiscal Year: 1992
    ..2) S- thiolation of proteins in susceptible cells results from exposure to either naphthalene (mediated by naphthoquinones) or 2-methylnaphthalene; 3) naphthalene oxides diffusing from metabolically active cells are capable of ..
  4. STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF DHAQ ANALOGS
    CHIA CHUNG CHENG; Fiscal Year: 1980
    ..synthesis of compounds of the following classes will be studied: (1) 9,10-anthraquinones, (2) 1,4-naphthoquinones and 1,4-benzoquinones, (3) quinones related to nogalamycin, (4) xanthones, thioxanthones, and acridones, and (..
  5. AZULOQUINONES: POTENTIAL NEW ANTITUMOR AGENTS
    LAWRENCE SCOTT; Fiscal Year: 1980
    ..Recent calculations predict that many of the azuloquinones will compare favorably to the known (isomeric) naphthoquinones in stability, reduction potential, etc...
  6. PLANT TUMOR INHIBITORS
    David Kingston; Fiscal Year: 1980
    ..The synthesis of some modified naphthoquinones as potential anticancer agents will also be carried out as a small portion of this project.
  7. MECHANISM OF ACTION OF ANTITUMOR DRUGS
    Leroy Liu; Fiscal Year: 1993
    ..shown to be a new class of topoisomerase I-targeting drugs; (2) investigate the mechanism(s) of action naphthoquinones and quinolones which may represent a new class(es) of topoisomerase II-targeting drugs...
  8. TOTAL SYNTHESIS OF THIOSTREPTON
    K Nicolaou; Fiscal Year: 2003
    ..The disease areas likely to benefit most from the proposed investigations are bacterial-caused diseases and malaria. ..
  9. TOTAL SYNTHESIS OF THIOSTREPTON
    K Nicolaou; Fiscal Year: 2002
    ..The disease areas likely to benefit most from the proposed investigations are bacterial-caused diseases and malaria. ..
  10. SYNTHESIS OF ANTIBIOTICS
    K Nicolaou; Fiscal Year: 2006
    ..unreadable] [unreadable]..
  11. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2006
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  12. TOTAL SYNTHESIS OF AZASPIRACIDS
    K Nicolaou; Fiscal Year: 2005
    ..g. lung, liver, spleen and lymphocyte damage as well as cancer) health hazards. The project is also expected to advance our knowledge in chemical synthesis and impact favorably the drug discovery and development process. ..
  13. TOTAL SYNTHESIS OF THIOSTREPTON
    K Nicolaou; Fiscal Year: 2005
    ..The disease areas likely to benefit most from the proposed investigations are bacterial-caused diseases and malaria. ..
  14. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2005
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  15. TOTAL SYNTHESIS OF THIOSTREPTON
    K Nicolaou; Fiscal Year: 2004
    ..The disease areas likely to benefit most from the proposed investigations are bacterial-caused diseases and malaria. ..
  16. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2004
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  17. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2003
    ..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
  18. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2003
    ..abstract_text> ..
  19. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
    ..abstract_text> ..
  20. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2004
    ..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
  21. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2004
    ..abstract_text> ..
  22. TOTAL SYNTHESIS OF AZASPIRACIDS
    K Nicolaou; Fiscal Year: 2006
    ..g. lung, liver, spleen and lymphocyte damage as well as cancer) health hazards. The project is also expected to advance our knowledge in chemical synthesis and impact favorably the drug discovery and development process. ..
  23. Synthesis of Marine Neurotoxins
    K C Nicolaou; Fiscal Year: 2010
    ..The project is also expected to significantly advance our knowledge in chemical synthesis, chemical biology, and medicine ..
  24. SYNTHESIS OF ANTIBIOTICS
    K C Nicolaou; Fiscal Year: 2010
    ..abstract_text> ..
  25. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
    ..abstract_text> ..
  26. Synthesis of Marine Neurotoxins
    K Nicolaou; Fiscal Year: 2009
    ..The project is also expected to significantly advance our knowledge in chemical synthesis, chemical biology, and medicine ..
  27. SYNTHESIS OF ANTIBIOTICS
    K Nicolaou; Fiscal Year: 2009
    ..abstract_text> ..
  28. SYNTHESIS OF ANTICANCER AGENTS
    K Nicolaou; Fiscal Year: 2009
    ..abstract_text> ..
  29. Synthesis of Marine Neurotoxins
    K Nicolaou; Fiscal Year: 2008
    ..The project is also expected to significantly advance our knowledge in chemical synthesis, chemical biology, and medicine ..
  30. SYNTHESIS OF ANTIBIOTICS
    K Nicolaou; Fiscal Year: 2008
    ..abstract_text> ..
  31. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2008
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  32. Synthesis of Marine Neurotoxins
    K Nicolaou; Fiscal Year: 2007
    ..The project is also expected to significantly advance our knowledge in chemical synthesis, chemical biology, and medicine ..
  33. TOTAL SYNTHESIS OF KINAMYCINS AND LOMAIVITICINS
    K Nicolaou; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  34. SYNTHESIS OF ANTIBIOTICS
    K Nicolaou; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  35. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2007
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  36. SYNTHESIS OF ANTICANCER AGENTS
    K Nicolaou; Fiscal Year: 2006
    ..unreadable] [unreadable] [unreadable]..
  37. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  38. SYNTHESIS OF ANTICANCER AGENTS
    K Nicolaou; Fiscal Year: 2008
    ..abstract_text> ..
  39. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2001
    ..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
  40. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2001
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  41. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 1999
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  42. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2002
    ..abstract_text> ..
  43. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2002
    ..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
  44. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2000
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  45. A Molecular Motor
    T Kelly; Fiscal Year: 2001
    ..The project should expand the understanding of chemically directed and controlled movement, which is a topic central to the understanding of biological systems. ..
  46. NOVEL APPROACHES TO ANTITUMOR AND ANTIVIRAL AGENTS
    BARRY TROST; Fiscal Year: 2004
    ..By accessing a very diverse range of structural types, the best opportunities to discover new therapeutic agents arise. ..
  47. NOVEL APPROACHES TO ANTITUMOR AND ANTIVIRAL AGENTS
    BARRY TROST; Fiscal Year: 2000
    ..Equally important, new avenues to vary structure around these cores in order to establish structure-activity relationships with the aim to create better therapeutic agents become available. ..
  48. NOVEL SYNTHETIC APPROACHES TO ANTITUMOR COMPOUNDS
    BARRY TROST; Fiscal Year: 1990
    ..A strategy to one family of tumor promoters represented by teleocidin explores the concept of chemical chameleons. In most cases, the strategy also considers the problem of absolute stereochemistry...
  49. Sterol Metabolism in Pneumocystis
    EDNA KANESHIRO; Fiscal Year: 2005
    ....
  50. SYNTHESIS OF MACROCYCLES STEROIDS CYCLOPENTANOIDS ETC
    BARRY TROST; Fiscal Year: 2000
    ..Ring expansion methods may convert these cores into the taxoid skeleton with appropriate functionality at key points for analog development. ..
  51. Sterol Metabolism in Pneumocystis
    EDNA KANESHIRO; Fiscal Year: 2006
    ....
  52. Synthesis of Macrolides. Steroids, Cyclopentanoids, etc
    BARRY TROST; Fiscal Year: 2003
    ..This new concept sets the stage for solutions to a long standing problem, the ion channel blockers, the grayanotoxins. as well as the more recently discovered rameswaralide, a potent antiinflamatory. ..
  53. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2007
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  54. A Molecular Motor
    T Kelly; Fiscal Year: 2002
    ..The project should expand the understanding of chemically directed and controlled movement, which is a topic central to the understanding of biological systems. ..
  55. NOVEL APPROACHES TO ANTITUMOR AND ANTIVIRAL AGENTS
    BARRY TROST; Fiscal Year: 2002
    ..By accessing a very diverse range of structural types, the best opportunities to discover new therapeutic agents arise. ..
  56. A Molecular Motor
    T Kelly; Fiscal Year: 2003
    ..The project should expand the understanding of chemically directed and controlled movement, which is a topic central to the understanding of biological systems. ..
  57. NOVEL SYNTHETIC APPROACHES TO ANTITUMOR COMPOUNDS
    BARRY TROST; Fiscal Year: 1992
    ..A strategy to one family of tumor promoters represented by teleocidin explores the concept of chemical chameleons. In most cases, the strategy also considers the problem of absolute stereochemistry...
  58. SYNTHESIS OF MACROCYCLES STEROIDS CYCLOPENTANOIDS ETC
    BARRY TROST; Fiscal Year: 2001
    ..Ring expansion methods may convert these cores into the taxoid skeleton with appropriate functionality at key points for analog development. ..
  59. THE SYNTHESIS OF LACTONAMYCIN AND ANALOGS
    T Kelly; Fiscal Year: 2000
    ..To test, in collaboration with Pfizer Inc., analogs and synthetic intermediates for antibiotic, anticancer and other biological activities. ..
  60. NOVEL APPROACHES TO ANTITUMOR AND ANTIVIRAL AGENTS
    BARRY TROST; Fiscal Year: 1993
    ..The diversity of the challenges posed by antiviral and antitumor agents represent highly meaningful tests of their use...
  61. PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTS
    Douglass Taber; Fiscal Year: 2007
    ..In the course of these investigations, new molecular reactivity will be developed that will substantially shorten current routes to polycyclic natural _roducts and drug candidates. ..
  62. Tissue Transglutaminase in Neurologic Injury
    THUNG SHEN LAI; Fiscal Year: 2007
    ..The inhibitors will be used to investigate the role of TTG in the pathogenesis of expanded polyQ diseases. Current proposal will lead to new therapy for HD and other neurologic disorders. [unreadable] [unreadable] [unreadable]..
  63. PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTS
    Douglass Taber; Fiscal Year: 2007
    ..In the course of these investigations, new molecular reactivity will be developed that will substantially shorten current routes to polycyclic natural products and drug candidates. ..
  64. PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTS
    Douglass Taber; Fiscal Year: 2006
    ..In the course of these investigations, new molecular reactivity will be developed that will substantially shorten current routes to polycyclic natural products and drug candidates. ..
  65. PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTS
    Douglass Taber; Fiscal Year: 2000
    ..Specific targets include the cognition-enhancing alkaloid huperzine A, morphine, the parent compound of the morphine alkaloids, and N-deacetyllappaconitine, representative of the Delphinium diterpenoid alkaloids. ..
  66. Cyanohydrin based fluorescent substrates of sEH (RMI)
    Christophe Morisseau; Fiscal Year: 2004
    ..This will be done by screening the combinatorial libraries from the "NIH Roadmap", libraries contracted from commercial vendors, and more defined libraries generated in house. ..
  67. PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTS
    Douglass Taber; Fiscal Year: 2005
    ..In the course of these investigations, new molecular reactivity will be developed that will substantially shorten current routes to polycyclic natural products and drug candidates. ..
  68. PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTS
    Douglass Taber; Fiscal Year: 2004
    ..In the course of these investigations, new molecular reactivity will be developed that will substantially shorten current routes to polycyclic natural products and drug candidates. ..
  69. PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTS
    Douglass Taber; Fiscal Year: 2002
    ..Specific targets include the cognition-enhancing alkaloid huperzine A, morphine, the parent compound of the morphine alkaloids, and N-deacetyllappaconitine, representative of the Delphinium diterpenoid alkaloids. ..
  70. PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTS
    Douglass Taber; Fiscal Year: 2001
    ..Specific targets include the cognition-enhancing alkaloid huperzine A, morphine, the parent compound of the morphine alkaloids, and N-deacetyllappaconitine, representative of the Delphinium diterpenoid alkaloids. ..
  71. PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTS
    Douglass Taber; Fiscal Year: 2003
    ..Specific targets include the cognition-enhancing alkaloid huperzine A, morphine, the parent compound of the morphine alkaloids, and N-deacetyllappaconitine, representative of the Delphinium diterpenoid alkaloids. ..
  72. ELLAGITANNIN AND RELATED CHEMISTRY
    Ken Feldman; Fiscal Year: 1999
    ..Finally new strategies for diasteroselective biaryl astropisomer assembly within the context of synthesis efforts directed toward the potent cytotoxic agent diazonamide A will extend current art in this area ..
  73. ELLAGITANNIN AND RELATED CHEMISTRY
    Ken Feldman; Fiscal Year: 2000
    ..Finally new strategies for diasteroselective biaryl astropisomer assembly within the context of synthesis efforts directed toward the potent cytotoxic agent diazonamide A will extend current art in this area ..
  74. Chemical and Biological Studies on Biaryl Phenolics
    Ken Feldman; Fiscal Year: 2004
    ..The search for selective 20S proteosome inhibitors among the Ntn-type proteases will be advanced by these investigations. ..
  75. New Methodology for Indole Alkaloid Syntheses
    Ken Feldman; Fiscal Year: 2008
    ..The use of a new variant of the Pummerer reaction to control both oxidation level and reaction site within the indole nucleus forms the basis of this chemistry. ..
  76. Chemical and Biological Studies on Biaryl Phenolics
    Ken Feldman; Fiscal Year: 2005
    ..The search for selective 20S proteosome inhibitors among the Ntn-type proteases will be advanced by these investigations. ..
  77. RADICAL MEDIATED CYCLIZATION REACTIONS
    Ken Feldman; Fiscal Year: 1993
    ..Successful completion of these syntheses will afford the targets (or analogs) in the most efficient manner to date...
  78. New Methodology for Indole Alkaloid Syntheses
    Ken Feldman; Fiscal Year: 2009
    ..The use of a new variant of the Pummerer reaction to control both oxidation level and reaction site within the indole nucleus forms the basis of this chemistry. ..
  79. ALKYNYLIODONIUM SALTS IN ORGANIC SYNTHESIS
    Ken Feldman; Fiscal Year: 2004
    ..Taken together, these studies will introduce new and concise techniques for preparing small polycyclic organic molecules of the type typically sought as pharmaceutical leads. ..
  80. Alkynyliodonium Salts and Derived Diyls in Synthesis
    Ken Feldman; Fiscal Year: 2005
    ..abstract_text> ..
  81. ALKYNYLIODONIUM SALTS IN ORGANIC SYNTHESIS
    Ken Feldman; Fiscal Year: 2000
    ..Taken together, these studies will introduce new and concise techniques for preparing small polycyclic organic molecules of the type typically sought as pharmaceutical leads. ..
  82. ELLAGITANNIN AND RELATED CHEMISTRY
    Ken Feldman; Fiscal Year: 2001
    ..Finally new strategies for diasteroselective biaryl astropisomer assembly within the context of synthesis efforts directed toward the potent cytotoxic agent diazonamide A will extend current art in this area ..
  83. New Methodology for Indole Alkaloid Syntheses
    Ken Feldman; Fiscal Year: 2007
    ..The use of a new variant of the Pummerer reaction to control both oxidation level and reaction site within the indole nucleus forms the basis of this chemistry. [unreadable] [unreadable]..