PLANT ANTITUMOR AGENTS

Summary

Principal Investigator: Kuo Hsiung Lee
Affiliation: University of North Carolina
Country: USA
Abstract: DESCRIPTION (verbatim from applicant's abstract): Based on continuing success and promising results in the previous grant period, the overall goal of the proposed research is to discover novel anticancer drugs from selected medicinal plants that have been chosen either for their therapeutic use to treat cancer(s) or for their novelty. Lead compounds will be isolated and identified based on cytotoxicity (human tissue culture cell line panel), mechanistic (DNA topoisomerase assays), and molecular target-based screening (androgen/androgen receptor target based assays). The identification and development of clinical trial candidates are overall goals of our program. The following specific studies will be carried out to accomplish these goals: 1) The Natural Products Laboratory (NPL) will use analytical instrumental chromatography to isolate and identify the active principles found in anticancer bioassays) termed bioactivity-directed fractionation and isolation, BDFI). The structural characterization of new active leads will be carried out by physical and spectral techniques. 2) Certain leads will be selected for structural modification and synthesis of analogs in order to elucidate their structure-activity relationships and mechanism of action as well as to improve their pharmacological profiles. Conventional structure activity relationship (SAR) studies, molecular modeling approaches, and combinatorial chemistry techniques are used by the NPL to aid lead generation and optimization. Current classes of primary interest include fluorinated phenyl quinolones, dithiophene and epipodophyllotoxin-camptothecin conjugates. 3) Promising compounds and their synthetic analogs will be submitted to the National Institutes of Health (NIH) at the National Cancer Institute (NCI) for additional in vitro and in vivo antitumor studies. Our previous program has been augmented by participation in the NCI Natural Product Repository Program (NCI-NPRP) for the study of promising cytotoxic rainforest species, and by the collaboration of Dr. C. S. Chang, University of Rochester Medical School, who has unique expertise in screening for prostate cancer targets. Our program continues to have the advantages of 1) an excellent supply of highly active lead compounds, (2) a focus on the structural modification of these new leads as clinical trials candidates, and (3) excellent productivity and a superior prospect for the successful development of a clinically useful drugs.
Funding Period: 1978-06-01 - 2005-05-31
more information: NIH RePORT

Top Publications

  1. ncbi Design, synthesis, and preclinical evaluation of new 5,6- (or 6,7-) disubstituted-2-(fluorophenyl)quinolin-4-one derivatives as potent antitumor agents
    Li Chen Chou
    Graduate Institute of Pharmaceutical Chemistry, China Medical University, Taichung, Taiwan
    J Med Chem 53:8047-58. 2010
  2. pmc Cytotoxic calanquinone A from Calanthe arisanensis and its first total synthesis
    Chia Lin Lee
    Natural Products Research Laboratories, School of Pharmacy, University of North Carolina at Chapel Hill, 315 Beard Hall, CB 7360, NC 27599 7360, USA
    Bioorg Med Chem Lett 18:4275-7. 2008
  3. pmc Cardiac glycosides from Antiaris toxicaria with potent cardiotonic activity
    Li Shian Shi
    Department of Chemistry, National Cheng Kung University, Tainan, Taiwan, Republic of China
    J Nat Prod 73:1214-22. 2010
  4. ncbi Sapinmusaponins F-J, bioactive tirucallane-type saponins from the galls of Sapindus mukorossi
    Hui Chi Huang
    Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan, Republic of China
    J Nat Prod 69:763-7. 2006
  5. pmc Altaicalarins A-D, cytotoxic bisabolane sesquiterpenes from Ligularia altaica
    Qi Wang
    Department of Pharmacognosy, School of Pharmacy, Fudan University, Shanghai 201203, People s Republic of China
    J Nat Prod 73:139-42. 2010
  6. pmc First total synthesis of protoapigenone and its analogues as potent cytotoxic agents
    An Shen Lin
    Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan
    J Med Chem 50:3921-7. 2007
  7. pmc Antitumor agents 287. Substituted 4-amino-2H-pyran-2-one (APO) analogs reveal a new scaffold from neo-tanshinlactone with in vitro anticancer activity
    Yizhou Dong
    Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599 7568, USA
    Bioorg Med Chem Lett 21:2341-4. 2011
  8. pmc New bichalcone analogs as NF-κB inhibitors and as cytotoxic agents inducing Fas/CD95-dependent apoptosis
    M Vijaya Bhaskar Reddy
    Department of Chemistry, National Cheng Kung University, Tainan 701, Taiwan
    Bioorg Med Chem 19:1895-906. 2011
  9. doi Synthesis, in vitro anti-inflammatory and cytotoxic evaluation, and mechanism of action studies of 1-benzoyl-β-carboline and 1-benzoyl-3-carboxy-β-carboline derivatives
    Mei Lin Yang
    Department of Chemistry, National Cheng Kung University, Tainan, Taiwan, ROC
    Bioorg Med Chem 19:1674-82. 2011
  10. pmc Antitumor agents 283. Further elaboration of desmosdumotin C analogs as potent antitumor agents: activation of spindle assembly checkpoint as possible mode of action
    Kyoko Nakagawa-Goto
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599 7568, USA
    Bioorg Med Chem 19:1816-22. 2011

Scientific Experts

  • Masuo Goto
  • Maurizio Bruno
  • J Koyama
  • D Colombo
  • K F Bastow
  • Kuo Hsiung Lee
  • Qian Shi
  • Hui Kang Wang
  • Pei Lin Wu
  • Masayuki Horiuchi
  • T Akihisa
  • Kyoko Nakagawa-Goto
  • Susan L Morris-Natschke
  • Yizhou Dong
  • Tian Shung Wu
  • Chin Yu Lai
  • Keduo Qian
  • Harukuni Tokuda
  • Xiaoming Yang
  • Tzu Hsuan Chen
  • Emika Ohkoshi
  • Yi Nan Liu
  • Yang Chang Wu
  • Che Ming Teng
  • Hsin Yi Hung
  • Sheng Chu Kuo
  • Fang Rong Chang
  • Shiow Lin Pan
  • Arnold Brossi
  • M Vijaya Bhaskar Reddy
  • Ernest Hamel
  • Jin Tatsuzaki
  • Qi Wang
  • Linyi Wei
  • Chia Lin Lee
  • Chung Ren Su
  • Donglei Yu
  • Chieh Yu Peng
  • Tsong Long Hwang
  • Xihong Wang
  • Pan Chyr Yang
  • Shuenn Chen Yang
  • Yuh Chiang Shen
  • Dao Feng Chen
  • Jau Chen Lin
  • Nobuko Sakurai
  • Chin Chung Wu
  • Hoyoku Nishino
  • Chihiro Ito
  • Xiao Feng Wang
  • Ping Chung Kuo
  • Amooru G Damu
  • Po Cheng Chiang
  • Hideji Itokawa
  • Chiao Ting Yen
  • Hsiu Hui Chan
  • Eva Y H P Lee
  • Li Shian Shi
  • Li Chen Chou
  • Mien Chie Hung
  • Yoshihide Usami
  • Li Jiau Huang
  • Masahiko Taniguchi
  • Sergio Rosselli
  • Shih Wei Wang
  • Li Lin
  • Seikou Nakamura
  • Lan Xie
  • Hao Zhu
  • Yoon Kim
  • Yojiro Sakurai
  • Elizabeth A Gullen
  • Yung Chi Cheng
  • Shwu Jen Wu
  • Sung Liang Yu
  • Takashi Kozaka
  • Jing Yu Lang
  • Mei Lin Yang
  • E Jian Lee
  • Yao Haur Kuo
  • Toshiyuki Akiyama
  • Makio Shibano
  • Hui Chi Huang
  • An Shen Lin
  • Mutsuo Kozuka
  • Masataka Itoigawa
  • Hiroshi Furukawa
  • Yan Lu
  • Sheng biao Wang
  • Min Chen

Detail Information

Publications119 found, 100 shown here

  1. ncbi Design, synthesis, and preclinical evaluation of new 5,6- (or 6,7-) disubstituted-2-(fluorophenyl)quinolin-4-one derivatives as potent antitumor agents
    Li Chen Chou
    Graduate Institute of Pharmaceutical Chemistry, China Medical University, Taichung, Taiwan
    J Med Chem 53:8047-58. 2010
    ..In summary, 15 is a promising clinical candidate and is currently under preclinical study...
  2. pmc Cytotoxic calanquinone A from Calanthe arisanensis and its first total synthesis
    Chia Lin Lee
    Natural Products Research Laboratories, School of Pharmacy, University of North Carolina at Chapel Hill, 315 Beard Hall, CB 7360, NC 27599 7360, USA
    Bioorg Med Chem Lett 18:4275-7. 2008
    ..The total synthesis of 1 was also achieved and is reported herein...
  3. pmc Cardiac glycosides from Antiaris toxicaria with potent cardiotonic activity
    Li Shian Shi
    Department of Chemistry, National Cheng Kung University, Tainan, Taiwan, Republic of China
    J Nat Prod 73:1214-22. 2010
    ..An electrophysiological recording showed that 23 inhibited the sodium pump current in a concentration-dependent manner...
  4. ncbi Sapinmusaponins F-J, bioactive tirucallane-type saponins from the galls of Sapindus mukorossi
    Hui Chi Huang
    Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan, Republic of China
    J Nat Prod 69:763-7. 2006
    ..Compounds 1-5 also showed moderate activity in a 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced Epstein-Barr virus early antigen (EBV-EA) activation assay...
  5. pmc Altaicalarins A-D, cytotoxic bisabolane sesquiterpenes from Ligularia altaica
    Qi Wang
    Department of Pharmacognosy, School of Pharmacy, Fudan University, Shanghai 201203, People s Republic of China
    J Nat Prod 73:139-42. 2010
    ..4, 0.8, 1.0, and 0.9 microg/mL, respectively...
  6. pmc First total synthesis of protoapigenone and its analogues as potent cytotoxic agents
    An Shen Lin
    Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan
    J Med Chem 50:3921-7. 2007
    ..Among them, 24 showed 2.2-14.2-fold greater cytotoxicity than 1 and naphthyl A-ring analogues remarkably enhanced the activity...
  7. pmc Antitumor agents 287. Substituted 4-amino-2H-pyran-2-one (APO) analogs reveal a new scaffold from neo-tanshinlactone with in vitro anticancer activity
    Yizhou Dong
    Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599 7568, USA
    Bioorg Med Chem Lett 21:2341-4. 2011
    ..Analogs 19, 20, 23, and 26-30 displayed significant tumor cell growth inhibitory activity in vitro. The most active compound 27 exhibited ED(50) values of 0.059-0.090 μM...
  8. pmc New bichalcone analogs as NF-κB inhibitors and as cytotoxic agents inducing Fas/CD95-dependent apoptosis
    M Vijaya Bhaskar Reddy
    Department of Chemistry, National Cheng Kung University, Tainan 701, Taiwan
    Bioorg Med Chem 19:1895-906. 2011
    ..70 to 13.10 μM. A mode of action study using HT-29 colon cancer cells showed that 23 acts by inducing apoptosis signaling...
  9. doi Synthesis, in vitro anti-inflammatory and cytotoxic evaluation, and mechanism of action studies of 1-benzoyl-β-carboline and 1-benzoyl-3-carboxy-β-carboline derivatives
    Mei Lin Yang
    Department of Chemistry, National Cheng Kung University, Tainan, Taiwan, ROC
    Bioorg Med Chem 19:1674-82. 2011
    ..Therefore, the synthetic 1-benzoyl-3-carboxy β-carboline analogs may have great potential to be developed as anti-inflammatory agents...
  10. pmc Antitumor agents 283. Further elaboration of desmosdumotin C analogs as potent antitumor agents: activation of spindle assembly checkpoint as possible mode of action
    Kyoko Nakagawa-Goto
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599 7568, USA
    Bioorg Med Chem 19:1816-22. 2011
    ..7 μM). The gene expression profiles showed that 3 may modulate the spindle assembly checkpoint (SAC) and chromosome separation, and thus, arrest cells at the G2/M-phase...
  11. ncbi Kalanchosides A-C, new cytotoxic bufadienolides from the aerial parts of Kalanchoe gracilis
    Pei Lin Wu
    Department of Cosmetic Science, Chung Hwa College of Medical Technology, Tainan 717, Taiwan, Republic of China
    Org Lett 8:5207-10. 2006
    ..All eight isolated compounds showed significant cytotoxic activity against a panel of human tumor cell lines, with potency reaching the nanomolar range. However, only bryophyllin B (8) inhibited HIV replication in H9 lymphocyte cells...
  12. pmc Discovery and development of natural product-derived chemotherapeutic agents based on a medicinal chemistry approach
    Kuo Hsiung Lee
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599 7568, USA
    J Nat Prod 73:500-16. 2010
    ..The discovery and development of these clinical trial candidates will also be discussed...
  13. pmc Antitumor agents. 274. A new synthetic strategy for E-ring SAR study of antofine and cryptopleurine analogues
    Xiaoming Yang
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599 7568, USA
    Org Lett 12:1416-9. 2010
    ..This strategy will greatly facilitate future SAR studies on the natural alkaloids with E-ring variations...
  14. pmc Antitumor agents. 256. Conjugation of paclitaxel with other antitumor agents: evaluation of novel conjugates as cytotoxic agents
    Kyoko Nakagawa-Goto
    Natural Products Research Laboratories, School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA
    Bioorg Med Chem Lett 17:2894-8. 2007
    ..These compounds also possessed anti-angiogenesis ability as well as lower inhibitory effects against a normal cell line (MRC-5). Thus, conjugates 8-10 are possible antitumor drug candidates, particularly for prostate cancer...
  15. ncbi Cytotoxic activity of some natural and synthetic ent-kauranes
    Sergio Rosselli
    Dipartimento di Chimica Organica, Universita di Palermo, Viale delle Scienze, 90128 Palermo, Italy
    J Nat Prod 70:347-52. 2007
    ..2 and 0.3 microM, respectively. These two 1-analogues are promising lead compounds for further investigation...
  16. pmc Biologically active constituents from the fruiting body of Taiwanofungus camphoratus
    Li Shian Shi
    Department of Biotechnology, National Formosa University, Yunlin 632, Taiwan
    Bioorg Med Chem 19:677-83. 2011
    ..camphoratus in traditional Chinese medicine (TCM) for the treatment of inflammation and cancer-related diseases. The newly discovered compounds deserve further development as anti-inflammatory candidates...
  17. pmc Antitumor agents 286. Design, synthesis, and structure-activity relationships of 3'R,4'R-disubstituted-2',2'-dimethyldihydropyrano[2,3-f]chromone (DSP) analogues as potent chemosensitizers to overcome multidrug resistance
    Ting Zhou
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599 7568, USA
    J Med Chem 53:8700-8. 2010
    ..Moreover, a preliminary mechanism study indicated that the chemosensitizing activity of DSP analogues results from inhibition of P-glycoprotein (P-gp) overexpressed in MDR cancer cells...
  18. pmc Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents
    Takashi Kozaka
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, NC 27599, USA
    Bioorg Med Chem Lett 20:4091-4. 2010
    ..0146 microg/mL) cells and the parent KB (0.0200 microg/mL) cell line...
  19. ncbi Cytotoxic Alangium alkaloids from Alangium longiflorum
    Nobuko Sakurai
    Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill, 27599, USA
    Phytochemistry 67:894-7. 2006
    ..The stereoisomer 1 was less potent than 2, and related compounds with different hydroxy/methoxy substitution patterns were also less potent or inactive. Thus, compound 2 merits attention as a cytotoxic lead for further study...
  20. pmc Antitumor agents 269. Non-aromatic ring-A neotanshinlactone analog, TNO, as a new class of potent antitumor agents
    Yizhou Dong
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA
    Bioorg Med Chem Lett 19:6289-92. 2009
    ..The cyclohexene ring-A could dramatically affect the antitumor activity and selectivity. Compound 20 showed the highest potency with ED(50) values of 0.7 and 1.7 microM against SK-BR-3 and ZR-75-1 breast cancer cell lines, respectively...
  21. pmc Songaricalarins A-E, cytotoxic oplopane sesquiterpenes from Ligularia songarica
    Qi Wang
    Department of Pharmacognosy, School of Pharmacy, Fudan University, Shanghai 201203, People s Republic of China
    J Nat Prod 76:305-10. 2013
    ..All compounds were evaluated for in vitro cytotoxic activity against cultured A-549, MCF-7, KB, and KBVIN cells, and 4 exhibited cytotoxicity with EC50 values of 4.9, 0.8, 3.4, and 3.2 μg/mL, respectively...
  22. pmc 1-(3,4,5-Trimethoxyphenyl)ethane-1,2-diyl esters, a novel compound class with potent chemoreversal activity
    Hsin Yi Hung
    Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599 7568, USA
    Bioorg Med Chem Lett 22:7726-9. 2012
    ..Further mechanism of action study showed 15 inhibited mainly P-glycoprotein efflux pump function, while 13 exhibited an additional multidrug resistance-associated protein efflux pump function...
  23. pmc Cryptopleurine analogs with modification of e ring exhibit different mechanism to rac-cryptopleurine and tylophorine
    Ying Wang
    Department of Pharmacology, Yale University School of Medicine, New Haven, CT, USA
    PLoS ONE 7:e51138. 2012
    ..Our results showed that DCB-3503 or Rac-cryptopleurine could be a scaffold for modification to yield compounds with different mechanisms of action...
  24. pmc Synthesis and biological evaluation of N-alkyl-N-(4-methoxyphenyl)pyridin-2-amines as a new class of tubulin polymerization inhibitors
    Xiao Feng Wang
    Beijing Institute of Pharmacology and Toxicology, 27 Tai Ping Road, Beijing 100850, PR China
    Bioorg Med Chem 21:632-42. 2013
    ..These promising results indicate that these tertiary diarylamine derivatives represent a novel class of tubulin polymerization inhibitors targeting the colchicine binding site and showing significant anti-proliferative activity...
  25. ncbi Neglschisandrins E-F: two new lignans and related cytotoxic lignans from Schisandra neglecta
    Min Chen
    Key Laboratory on Luminescence and Real Time Analysis Ministry of Education, College of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China
    Molecules 18:2297-306. 2013
    ..33~19.8 μg/mL. In addition, compounds 2-4 also exhibited marginal cytotoxicity against the human lung carcinoma A549 cell line with EC₅₀ values of 11.8~15.0 μg/mL...
  26. pmc N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines: a novel class of antitumor agents targeting the colchicine site on tubulin
    Xiao Feng Wang
    Beijing Institute of Pharmacology and Toxicology, 27 Tai Ping Road, Beijing 100850, China Pharmacy Department, Urumqi General Hospital, Lanzhou Military Region, Urumqi 830000, China
    Eur J Med Chem 67:196-207. 2013
    ..Related SAR analysis, molecular modeling, and evaluation of essential drug-like properties, i.e. water solubility, log P, and in vitro metabolic stability, were also performed. ..
  27. pmc Antitumor agents 295. E-ring hydroxylated antofine and cryptopleurine analogues as antiproliferative agents: design, synthesis, and mechanistic studies
    Xiaoming Yang
    Natural Products Research Laboratories and Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599 7568, United States
    J Med Chem 55:6751-61. 2012
    ..Mechanistic studies revealed that 13b is able to down-regulate HSP90 and β-catenin in A549 lung adenocarcinoma cells in a dose-dependent manner, suggesting a potential use for treating hedgehog pathway-driven tumorigenesis...
  28. doi Cytotoxic and potential anticancer constituents from the stems of Schisandra pubescens
    Yan Lu
    Department of Pharmacognosy, School of Pharmacy, Fudan University, Shanghai, P R China
    Pharm Biol 51:1204-7. 2013
    ..The diethyl ether extract of the stems of Schisandra pubescens Hemsl. et Wils. (Schisandraceae) was found to exhibit cytotoxic activity in vitro. However, investigations of the bioactive constituents of this plant have been very limited...
  29. pmc Antitumor agents 294. Novel E-ring-modified camptothecin-4β-anilino-4'-O-demethyl-epipodophyllotoxin conjugates as DNA topoisomerase I inhibitors and cytotoxic agents
    Deyong Ye
    Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599 7568, USA
    Bioorg Med Chem 20:4489-94. 2012
    ..The novel structures of 1E and 2E may present scaffolds for further development of dual function topo I and II inhibitors with improved pharmacological profiles and physicochemical properties...
  30. doi Cancer preventive agents 11. Novel analogs of dimethyl dicarboxylate biphenyl as potent cancer chemopreventive agents(†)
    Hsin Yi Hung
    Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599 7568, USA
    Pharm Biol 50:18-24. 2012
    ..Dimethyl dicarboxylate biphenyl (DDB) is a clinically used hepatoprotectant and has also been found to have chemopreventive activity...
  31. pmc Antitumor agents. 272. Structure-activity relationships and in vivo selective anti-breast cancer activity of novel neo-tanshinlactone analogues
    Yizhou Dong
    Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, North Carolina 27599, USA
    J Med Chem 53:2299-308. 2010
    ..Further development of lead compounds 19-21 and 24 as clinical trial candidates is warranted...
  32. pmc Antitumor agents. 266. Design, synthesis, and biological evaluation of novel 2-(furan-2-yl)naphthalen-1-ol derivatives as potent and selective antibreast cancer agents
    Yizhou Dong
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA
    J Med Chem 52:3586-90. 2009
    ..Further optimization led to 18 and 21, which showed decreased cytotoxic potency but better selectivity than neo-tanshinlactone analogue 2. Interestingly, 20 showed broad cytotoxicity against human cancer cell lines...
  33. pmc Antitumor agents. 289. Design, synthesis, and anti-breast cancer activity in vivo of 4-amino-2H-benzo[h]chromen-2-one and 4-amino-7,8,9,10-tetrahydro-2H-benzo[h]chromen-2-one analogues with improved water solubility
    Yizhou Dong
    Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599 7568, United States
    J Nat Prod 75:370-7. 2012
    ..Compound 10 merits further development as a promising anticancer clinical trial candidate...
  34. pmc Design and synthesis of gambogic acid analogs as potent cytotoxic and anti-inflammatory agents
    Chiao Ting Yen
    Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, NC 27599 7568, USA
    Bioorg Med Chem Lett 22:4018-22. 2012
    ..9 and 0.8 μg/mL, respectively. An angular 3-methyl-3-prenylpyranoxanthone (17) selectively inhibited elastase release with 200 times more potency than phenylmethylsulfonyl fluoride (PMSF), the positive control...
  35. pmc Antitumor agents. 293. Nontoxic dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethylenedioxybiphenyl-2,2'-dicarboxylate (DDB) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs
    Hsin Yi Hung
    Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599 7568, United States
    J Med Chem 55:5413-24. 2012
    ..The mechanism of action studies demonstrated that effective inhibition of P-glycoprotein by DDB analogues dramatically elevated the cellular concentration of anticancer drugs...
  36. pmc Antitumor agents 290. Design, synthesis, and biological evaluation of new LNCaP and PC-3 cytotoxic curcumin analogs conjugated with anti-androgens
    Qian Shi
    Natural Products Research Laboratories, UNC Eshelmen School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599 7568, USA
    Bioorg Med Chem 20:4020-31. 2012
    ..The evidence suggests that distinguishable target proteins are involved, resulting in the different outcomes toward pseudopodia suppression...
  37. pmc Antitumor agents 270. Novel substituted 6-phenyl-4H-furo[3,2-c]pyran-4-one derivatives as potent and highly selective anti-breast cancer agents
    Yizhou Dong
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599 7568, United States
    Bioorg Med Chem 18:803-8. 2010
    ..In addition, 25 displayed low cytotoxicity against normal breast cell lines 184A1 and MCF10A. Compounds 25 and 27 merit further investigation in our continuing program to generate and develop selective anti-breast cancer agents...
  38. pmc Cytotoxic polyisoprenyl benzophenonoids from Garcinia subelliptica
    Li Jie Zhang
    National Research Institute of Chinese Medicine, Taipei 112, Taiwan, Republic of China
    J Nat Prod 73:557-62. 2010
    ..Biological evaluation showed that all compounds 1-9 exhibited cytotoxic activity against a small panel of human tumor cell lines (A549, DU145, KB, vincristine-resistant KB)...
  39. pmc Antitumor agents 268. Design, synthesis, and mechanistic studies of new 9-substituted phenanthrene-based tylophorine analogues as potent cytotoxic agents
    Xiaoming Yang
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599 7568, USA
    J Med Chem 52:5262-8. 2009
    ....
  40. pmc Antitumor agents 278. 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs as potent in vitro anti-cancer agents
    Yizhou Dong
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599 7568, United States
    Bioorg Med Chem Lett 20:4085-7. 2010
    ..01-76 microM. Preliminary SAR results indicated that substitutions on nitrogen are critical to the antitumor potency...
  41. pmc Cancer preventive agents 10. Prenylated dehydrozingerone analogs as potent chemopreventive agents
    Jin Tatsuzaki
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC, USA
    J Asian Nat Prod Res 12:227-32. 2010
    ..Because in vitro inhibitory effects in this assay generally correlate well with in vivo inhibitory effects on tumor promotion, our results strongly suggested that prenylated 16 and 34-36 are likely to be promising antitumor promoters...
  42. pmc Antitumor agents. 280. Multidrug resistance-selective desmosdumotin B analogues
    Kyoko Nakagawa-Goto
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, USA
    J Med Chem 53:6699-705. 2010
    ..While 2-4 showed either no or very weak inhibition of cellular P-glycoprotein (P-gp) activity, they either activated or inhibited the actions of the first generation P-gp inhibitors verapamil or cyclosporin, respectively...
  43. pmc Antitumor Agents. 282. 2'-(R)-O-acetylglaucarubinone, a quassinoid from Odyendyea gabonensis as a potential anti-breast and anti-ovarian cancer agent
    Yoshihide Usami
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599 7568, USA
    J Nat Prod 73:1553-8. 2010
    ..When tested against mammary epithelial proliferation in vivo using a Brca1/p53-deficient mice model, 1 also caused significant reduction in mammary duct branching...
  44. doi Antitumor agents 292. Design, synthesis and pharmacological study of S- and O-substituted 7-mercapto- or hydroxy-coumarins and chromones as potent cytotoxic agents
    Ying Chen
    Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, China
    Eur J Med Chem 49:74-85. 2012
    ..Thus, these coumarin derivatives merit investigation as novel potential antitumor agents with further structural modification to produce an optimal lead compound and elucidate the detailed pharmacological mechanism(s)...
  45. pmc Cytotoxic esterified diterpenoid alkaloid derivatives with increased selectivity against a drug-resistant cancer cell line
    Koji Wada
    Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599 7568, USA
    Bioorg Med Chem Lett 22:249-52. 2012
    ..6-Acylation of 1 appears to be critical for producing cytotoxic activity in this alkaloid class and a means to provide promising new leads for further development into antitumor agents...
  46. doi Bis-chalcone analogues as potent NO production inhibitors and as cytotoxic agents
    M Vijaya Bhaskar Reddy
    Department of Chemistry, National Cheng Kung University, Tainan 701, Taiwan, ROC
    Eur J Med Chem 47:97-103. 2012
    ..Structure-activity relationship (SAR) findings are also discussed...
  47. pmc ortho-Quinone tanshinones directly inhibit telomerase through an oxidative mechanism mediated by hydrogen peroxide
    Joana Soares
    Eshelman School of Pharmacy, Division of Chemical Biology and Medicinal Chemistry, University of North Carolina, Chapel Hill, NC 27599 7568, USA
    Bioorg Med Chem Lett 21:7474-8. 2011
    ..The results also provide evidence that telomerase is directly and negatively regulated by reactive oxygen species...
  48. ncbi Dyscusins A-C, three new steroids from the leaves of Dysoxylum cumingianum
    Shin ichiro Kurimoto
    Graduate School of Pharmaceutical Sciences, University of Tokushima, Tokushima, Japan
    Chem Pharm Bull (Tokyo) 59:1303-6. 2011
    ..5 µM colchicine as compared with the absence of colchicine. This notable finding indicated that 1 possessed a multi-drug resistant reversal effect...
  49. pmc Bioactive constituents from the roots of Panax japonicus var. major and development of a LC-MS/MS method for distinguishing between natural and artifactual compounds
    Hsiu Hui Chan
    Department of Chemistry, National Cheng Kung University, 1 Ta Hsueh Road, Tainan 70101, Taiwan
    J Nat Prod 74:796-802. 2011
    ..78 to 43.6 μM. In addition, 1 showed greater than 2- to 3-fold selective cytotoxic activity against KB and DU145 cancer cell lines...
  50. pmc Antitumor agents. 284. New desmosdumotin B analogues with bicyclic B-ring as cytotoxic and antitubulin agents
    Kyoko Nakagawa-Goto
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States
    J Med Chem 54:1244-55. 2011
    ..Furthermore, 21 inhibited tubulin assembly in vitro with an IC(50) value of 2.0 μM and colchicine binding by 78% as well as cellular microtubule polymerization and spindle formation...
  51. pmc Antitumor agents 288: design, synthesis, SAR, and biological studies of novel heteroatom-incorporated antofine and cryptopleurine analogues as potent and selective antitumor agents
    Xiaoming Yang
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599 7568, USA
    J Med Chem 54:5097-107. 2011
    ..Compound 11 also showed greatly reduced cytotoxicity against normal cells and moderate antitumor activity against HT-29 human colorectal adenocarcinoma xenograft in mice without overt toxicity...
  52. pmc Camphoratins A-J, potent cytotoxic and anti-inflammatory triterpenoids from the fruiting body of Taiwanofungus camphoratus
    Shwu Jen Wu
    Department of Medical Technology, Chung Hua University of Medical Technology, Tainan 717, Taiwan, Republic of China
    J Nat Prod 73:1756-62. 2010
    ..Compounds 6, 10, 11, 14-16, 18, and 21 exhibited anti-inflammatory NO-production inhibition activity with IC(50) values of less than 5 μM, and were more potent than the nonspecific NOS inhibitor N(ω)-nitro-L-arginine methyl ester...
  53. pmc Antitumor agents 281. Design, synthesis, and biological activity of substituted 4-amino-7,8,9,10-tetrahydro-2H-benzo[h]chromen-2-one analogs (ATBO) as potent in vitro anticancer agents
    Yizhou Dong
    Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599 7568, USA
    Bioorg Med Chem Lett 21:546-9. 2011
    ..Compound 15 was the most potent analog compared with structurally related neo-tanshinlactone (e.g., 1) and 4-amino-2H-benzo[h]chromen-2-one (ABO, e.g., 4) analogs, and thus merits further exploration as an anti-cancer drug candidate...
  54. pmc Antitumor agents 279. Structure-activity relationship and in vivo studies of novel 2-(furan-2-yl)naphthalen-1-ol (FNO) analogs as potent and selective anti-breast cancer agents
    Yizhou Dong
    Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599 7568, USA
    Bioorg Med Chem Lett 21:52-7. 2011
    ..Treatment with 3 in Brca1(f11/f11)p53(f5&6/f5&6)Cre(c) mice models significantly inhibited the proliferation of mammary epithelial cells and branching of mammary glands...
  55. doi Biosynthesis, total syntheses, and antitumor activity of tanshinones and their analogs as potential therapeutic agents
    Yizhou Dong
    Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599 7568, USA
    Nat Prod Rep 28:529-42. 2011
    ..This review will discuss the biosynthesis, total syntheses, and antitumor activities of tanshinones,especially neo-tanshinlactone and its analogs...
  56. pmc Antitumor agents. 271: total synthesis and evaluation of brazilein and analogs as anti-inflammatory and cytotoxic agents
    Chiao Ting Yen
    Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, NC 27599 7568, USA
    Bioorg Med Chem Lett 20:1037-9. 2010
    ..Additionally, 1b exhibited broad spectrum in vitro anticancer activity with IC(50) values of 6-11 microM against the four tested cancer cell lines...
  57. doi Synthesis and preclinical evaluations of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na) as a potent antitumor agent
    Li Chen Chou
    Graduate Institute of Pharmaceutical Chemistry, China Medical University, Taichung, Taiwan
    J Med Chem 53:1616-26. 2010
    ..With excellent antitumor activity profiles, 4 is highly promising for development as an anticancer clinical trials candidate...
  58. pmc Design and synthesis of 2-(3-benzo[b]thienyl)-6,7-methylenedioxyquinolin-4-one analogues as potent antitumor agents that inhibit tubulin assembly
    Yu Hsun Chang
    Graduate Institute of Pharmaceutical Chemistry, China Medical University, Taichung, Taiwan
    J Med Chem 52:4883-91. 2009
    ..07 and 0.19 microM. Results from mechanism of action studies revealed that these new quinolone derivatives function as antitubulin agents...
  59. ncbi Novel anti-prostate cancer curcumin analogues that enhance androgen receptor degradation activity
    Q Shi
    AndroScience Corporation, San Diego, CA, 91121, USA
    Anticancer Agents Med Chem 9:904-12. 2009
    ..These compounds, such as ASC-J9 and its analogues (3 and 4), have now been shown to inhibit prostate cancer proliferation through a novel mechanism of enhancing AR degradation...
  60. ncbi The cytotoxic properties of natural coumarins isolated from roots of Ferulago campestris (Apiaceae) and of synthetic ester derivatives of aegelinol
    Sergio Rosselli
    Dipartimento Chimica Organica E Paternò, Universita di Palermo, Viale delle Scienze, Parco d Orleasn II, 90128 Palermo, Italy
    Nat Prod Commun 4:1701-6. 2009
    ..Some of them were shown to be marginally cytotoxic against the A549 lung cancer cell line...
  61. ncbi Correlation between reduction potentials and inhibitory effects on Epstein-Barr virus activation by emodin derivatives
    Junko Koyama
    Faculty of Pharmaceutical Sciences, Kobe Pharmaceutical University, Higashinada, Kobe 658 8558, Japan
    Cancer Lett 241:263-7. 2006
    ..The electronic properties, i.e. LUMO energy and atomic charges of carbon at the 9-position (C(9)) and oxygen at the 11-position (O(11)), may also be useful for estimating the inhibitory effect on EBV-EA activation...
  62. doi Anti-HBV and cytotoxic activities of pyranocoumarin derivatives
    Chung Ren Su
    Department of Chemistry, National Cheng Kung University, Tainan, Taiwan
    Bioorg Med Chem 17:6137-43. 2009
    ..These data suggest that these three compounds could be useful hits for developing MDR-inverse drugs...
  63. ncbi Antitumor agents. Part 236: Synthesis of water-soluble colchicine derivatives
    Kyoko Nakagawa-Goto
    Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA
    Bioorg Med Chem Lett 15:235-8. 2005
    ..88 microg/mL. The thiocolchicine analogs (5, 5a) were more potent than the colchicine analogs (4, 4a) in the tubulin polymerization assay. In particular, the water-soluble salt 5a merits preclinical development as an antitumor agent...
  64. ncbi Antitumor agents 247. New 4-ethoxycarbonylethyl curcumin analogs as potential antiandrogenic agents
    Li Lin
    Natural Products Laboratory, School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599 7360, USA
    Bioorg Med Chem 14:2527-34. 2006
    ..Among them, compound 10 was found to be the most potent anti-AR agent and is considered to be a promising drug candidate for the treatment of prostate cancer...
  65. ncbi Chalcones and other compounds from the exudates of Angelica keiskei and their cancer chemopreventive effects
    Toshihiro Akihisa
    College of Science and Technology, Nihon University, 1 8 Kanda Surugadai, Tokyo 101 8308, Japan
    J Nat Prod 69:38-42. 2006
    ..Further, isobavachalcone (4) exhibited inhibitory effects on skin tumor promotion in an in vivo two-stage mouse skin carcinogenesis test using 7,12-dimethylbenz[a]anthracene (DMBA) as an initiator and TPA as a promoter...
  66. ncbi Three new agarofuran sesquiterpenes reissantins F-H from Reissantia buchananii
    Fang Rong Chang
    Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung, Taiwan
    Planta Med 72:92-6. 2006
    ..Their structures as well as their relative stereochemistry were established on the basis of modern mass and spectroscopic methods. Compounds were assayed for cytotoxicity against HepG2 and Hep3B human liver cancer cell lines...
  67. ncbi Sylviside, a diterpene glucoside derivative from Gnaphalium sylvaticum
    Mira M Konopleva
    Department of Pharmacognosy and Botany, Vitebsk State University, Republic of Belarus
    J Nat Prod 69:394-6. 2006
    ..Sylviside (1) displayed weak cytotoxicity against HeLa WT (human epitheloid cervical carcinoma) cells and was also evaluated for its effects on reversing multidrug resistance in HeLa cells overexpressing MDR1...
  68. ncbi Rautandiols A and B, pterocarpans and cytotoxic constituents from Neorautanenia mitis
    Yojiro Sakurai
    Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill, 27599, USA
    J Nat Prod 69:397-9. 2006
    ..Among the compounds isolated, rotenone (3) and 12-hydroxyrotenone (4) showed significant cytotoxic activity with IC(50) values of 0.008-0.010 and 0.04-0.06 microg/mL against MCF-7 and A-549 cells, respectively...
  69. pmc Antitumor agents. 250. Design and synthesis of new curcumin analogues as potential anti-prostate cancer agents
    Li Lin
    Natural Products Laboratory, School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599 7360, USA
    J Med Chem 49:3963-72. 2006
    ..This study established an advanced structure-activity relationship (SAR), and these correlations will guide the further design of new curcumin analogues with better anti-prostate cancer activity...
  70. ncbi Antitumor agents 251: synthesis, cytotoxic evaluation, and structure-activity relationship studies of phenanthrene-based tylophorine derivatives (PBTs) as a new class of antitumor agents
    Linyi Wei
    Natural Products Research Laboratories, School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA
    Bioorg Med Chem 14:6560-9. 2006
    ..16 and 0.27 microM, respectively, which are comparable to those of currently used antitumor drugs. A structure-activity relationship (SAR) study was also explored to facilitate the further development of this new compound class...
  71. ncbi New developments in the chemistry and biology of the bioactive constituents of Tanshen
    Xihong Wang
    Natural Products Research Laboratories, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, USA
    Med Res Rev 27:133-48. 2007
    ..This compound might serve as a lead for developing promising antibreast cancer clinical trials candidates...
  72. ncbi Antitumor agents. 254. Synthesis and biological evaluation of novel neo-tanshinlactone analogues as potent anti-breast cancer agents
    Xihong Wang
    Natural Products Research Laboratories, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, USA
    J Med Chem 49:5631-4. 2006
    ..Our preliminary SAR studies showed that a methylated furan ring D and the C-4 substituent in ring A are critical for anti-breast cancer activity. Further development of 1 and 15 as anti-breast cancer drug candidates is warranted...
  73. ncbi Tripfordines A-C, sesquiterpene pyridine alkaloids from Tripterygium wilfordii, and structure anti-HIV activity relationships of Tripterygium alkaloids
    Masafumi Horiuch
    Department of Interdisciplinary Studies of Natural Environment, Faculty of Integrated Arts and Sciences, Hiroshima University, Higashi hiroshima 739 8521, Japan
    J Nat Prod 69:1271-4. 2006
    ..1 microg/mL). In contrast, a hydroxy group at C-8' (carboxypropyl side chain) or C-9' (carboxybutyl side chain) was found to affect anti-HIV activity...
  74. ncbi Cyclic and branched acyl chain galactoglycerolipids and their effect on anti-tumor-promoting activity
    Diego Colombo
    Dipartimento di Chimica, Biochimica e Biotecnologie per la Medicina, Universita di Milano, Via Saldini 50, 20133 Milano, MI, Italy
    Eur J Med Chem 41:1456-63. 2006
    ....
  75. ncbi Cytotoxic activity of some natural and synthetic sesquiterpene lactones
    Maurizio Bruno
    Dipartimento di Chimica Organica, Universita di Palermo, Palermo, Italy
    Planta Med 71:1176-8. 2005
    ..Elemane, heliangolane and their hydroxy analogues 9 and 10, all containing an alpha,beta-unsaturated aldehyde substituent, were the most potent compounds...
  76. ncbi Porritoxins, metabolites of Alternaria porri, as anti-tumor-promoting active compounds
    Masayuki Horiuchi
    Research Institute for Production Development, Sakyo ku, Kyoto 606 0805, Japan
    Nat Prod Res 20:161-6. 2006
    ..Inhibitory effect of porritoxin (1) and (2) was superior to that of beta-carotene, a well-known anti-tumor promoter. Furthermore, the structure-activity correlation of porritoxins and their related compounds were discussed...
  77. ncbi Cytotoxic activity of some natural and synthetic guaianolides
    Maurizio Bruno
    Dipartimento di Chimica Organica, Universita di Palermo, Viale delle Scienze, 90128 Palermo, Italy
    J Nat Prod 68:1042-6. 2005
    ..Repin (1) and both mono- and di-halohydrin analogues (2, 7-9, 11, 12) showed significant antitumor potency. A more effective compound (17) was obtained by esterificating repin with the paclitaxel side chain...
  78. ncbi Synthesis and biological relationships of 3',6-substituted 2-phenyl-4-quinolone-3-carboxylic acid derivatives as antimitotic agents
    Ya Yun Lai
    Graduate Institute of Pharmaceutical Chemistry, China Medical University, Taichung, Taiwan
    Bioorg Med Chem 13:265-75. 2005
    ..The mechanism of action may be similar, but not identical, to that of tubulin binding drugs, such as navelbine and taxol. Compound 68 merits further investigation as a novel hydrophilic antimitotic agent...
  79. ncbi Anti-tumor-promoting activity of simple models of galactoglycerolipids with branched and unsaturated acyl chains
    Diego Colombo
    Dipartimento di Chimica, Biochimica e Biotecnologie per la Medicina, Universita di Milano, Via Saldini 50, 20133 Milano, Italy
    Eur J Med Chem 40:69-74. 2005
    ..Four compounds (three butenoates and one 4-methylpentanoate), when tested in the in vivo two-stage carcinogenesis test, exhibited also inhibitory effects on mouse skin tumor promotion...
  80. ncbi Cancer preventive agents. Part 1: chemopreventive potential of cimigenol, cimigenol-3,15-dione, and related compounds
    Nobuko Sakurai
    Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599 7360, USA
    Bioorg Med Chem 13:1403-8. 2005
    ..Thus, compounds 1 and 2 exhibited not only strong antitumor-promoting activity but also significant antitumor-initiating effect on mouse skin. These data suggest that both compounds might be valuable chemopreventors...
  81. ncbi Antitumor-promoting activity of coumarins from citrus plants
    Chihiro Ito
    Faculty of Pharmacy, Meijo University, Tempaku, Nagoya, Japan
    Planta Med 71:84-7. 2005
    ..Osthenol (7) exhibited a marked inhibitory effect on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test...
  82. ncbi Chemical constituents of Murraya siamensis: three coumarins and their anti-tumor promoting effect
    Chihiro Ito
    Faculty of Pharmacy, Meijo University, Tempaku, Nagoya 468 8503, Japan
    Phytochemistry 66:567-72. 2005
    ..Results of a primary screening of inhibitory effects of seven of these compounds on 12-O-tetradecanoylphorbol-13-acetate-induced Epstein-Barr virus early antigen activation in Raji cells are also presented...
  83. ncbi Antitumor agents 243. Syntheses and cytotoxicity of desmosdumotin C derivatives
    Kyoko Nakagawa-Goto
    Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA
    Bioorg Med Chem 13:2325-30. 2005
    ..Compounds 2-9, 13, and 16 were evaluated in vitro against human tumor cell replication. The 4-bromophenyl analog (2) showed potent cytotoxic activity in four different tumor cell lines...
  84. ncbi LC/TIS-MS fingerprint profiling of Cimicifuga species and analysis of 23-Epi-26-deoxyactein in Cimicifuga racemosa commercial products
    Hui Kang Wang
    AndroScience Corporation, 11175 Flintkote Avenue, Suite F, San Diego, California 92121, USA
    J Agric Food Chem 53:1379-86. 2005
    ....
  85. ncbi Intercedensides D-I, cytotoxic triterpene glycosides from the sea cucumber Mensamaria intercedens Lampert
    Zhengrong Zou
    Research Center for Marine Drugs, School of Pharmacy, Second Military Medical University, 325 Guo He Road, Shanghai 200433, People s Republic of China
    J Nat Prod 68:540-6. 2005
    ..lntercedensides D-H (1-5) showed significant cytotoxicity (ED(50) 0.96-5.0 mug/mL) against 10 human tumor cell lines...
  86. ncbi Cancer preventive agents, Part 2: Synthesis and evaluation of 2-phenyl-4-quinolone and 9-oxo-9,10-dihydroacridine derivatives as novel antitumor promoters
    Seikou Nakamura
    Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA
    Bioorg Med Chem 13:4396-401. 2005
    ....
  87. ncbi Novel cytotoxic monotetrahydrofuranic Annonaceous acetogenins from Annona montana
    Chih Chuang Liaw
    Graduate Institute of Natural Products, Kaohsiung Medical University, 100, Shih Chuan 1st Road, Kaohsiung, Taiwan
    Bioorg Med Chem 13:4767-76. 2005
    ..The absolute stereochemical structures of new isolates were elucidated and characterized by spectral and chemical methods. Interestingly, these compounds show special cytotoxicity against human hepatoma cells, Hep G2...
  88. ncbi Correlation between reduction potentials and inhibitory effects on Epstein-Barr virus activation of poly-substituted anthraquinones
    Junko Koyama
    Faculty of Pharmaceutical Sciences, Kobe Pharmaceutical University, Higashinada, Kobe 658 8558, Japan
    Cancer Lett 225:193-8. 2005
    ..It has been further shown that the correlation can be enhanced by introducing log P as an additional parameter...
  89. pmc Dehydrozingerone, chalcone, and isoeugenol analogues as in vitro anticancer agents
    Jin Tatsuzaki
    Natural Products Research Laboratories, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599 7360, USA
    J Nat Prod 69:1445-9. 2006
    ..0, 1.0, and 2.0 microg/mL, respectively) and KB-VCR (IC50 values of 1.9, 1.0, and 2.0 microg/mL, respectively) cells, suggesting that they are not substrates for the P-glycoprotein drug efflux pump...
  90. ncbi Antitumor-promoting effects of new sesquiterpenes from Crossopetalum tonduzii
    Cristina R Mendoza
    Instituto Universitario de Bio Organica Antonio Gonzalez, Universidad de La Laguna, Avenida Astrofisico Francisco Sanchez 2, La Laguna, 38206 Tenerife
    Chem Biodivers 2:286-94. 2005
    ..The new compounds showed moderate antitumor-promoting effects with respect to the activation of the Epstein-Barr virus early antigen (EBV-EA)...
  91. ncbi Synthetic cinnamylphenol derivatives as cancer chemopreventive agents
    Chihiro Ito
    Faculty of Pharmacy, Meijo University, Tempaku ku, Nagoya 468 8503, Japan
    Eur J Med Chem 42:902-9. 2007
    ..These results indicate that some prenylated cinnamylphenols might be valuable as potential cancer chemopreventive agents (anti-tumor promoters)...
  92. doi Antitumor agents. 261. 20(S)-protopanaxadiol and 20(s)-protopanaxatriol as antiangiogenic agents and total assignment of (1)H NMR spectra
    Yoshihide Usami
    School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599 7360, USA
    J Nat Prod 71:478-81. 2008
    ..This report is the first to completely assign the (1)H NMR signals of 2, together with correction of data for 1 from prior reports...
  93. doi CHM-1, a novel synthetic quinolone with potent and selective antimitotic antitumor activity against human hepatocellular carcinoma in vitro and in vivo
    Shih Wei Wang
    Pharmacological Institute, College of Medicine, National Taiwan University, Taipei, Taiwan
    Mol Cancer Ther 7:350-60. 2008
    ..CHM-1 is a promising chemotherapeutic agent worthy of further development into a clinical trial candidate for treating cancer, especially hepatocellular carcinoma...
  94. doi Plant-derived natural product research aimed at new drug discovery
    Hideji Itokawa
    Natural Products Research Laboratories, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599 7360, USA
    J Nat Med 62:263-80. 2008
    ....
  95. pmc Total synthesis of phenanthroindolizidine alkaloids (+/-)-antofine, (+/-)-deoxypergularinine, and their dehydro congeners and evaluation of their cytotoxic activity
    Chung Ren Su
    Department of Chemistry, National Cheng Kung University, Tainan 701, Taiwan, ROC
    Bioorg Med Chem 16:6233-41. 2008
    ..Increasing the planarity and rigidity of the indolizidine moiety significantly reduced potency. A methoxy group at the 2-position (1a) was more favorable for cytotoxic activity than a hydrogen atom (1b)...
  96. doi Antitumor agents 260. New desmosdumotin B analogues with improved in vitro anticancer activity
    Kyoko Nakagawa-Goto
    Natural Products Research Laboratories, School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA
    J Med Chem 51:3297-303. 2008
    ..Thus, 1-analogues might be a new class of potent drug candidates, especially as 11 and 12 express direct selective action against tumors expressing MDR...
  97. pmc Synthesis and proteasome inhibition of glycyrrhetinic acid derivatives
    Li Huang
    Department of Surgery, Box 2926, Duke University Medical Center, Durham, NC 27710 2926, USA
    Bioorg Med Chem 16:6696-701. 2008
    ..Among the derivatives, glycyrrhetinic acid 3-O-isophthalate (17) was the most potent compound with IC(50) of 0.22microM, which was approximately 100-fold more potent than glycyrrhetinic acid...
  98. ncbi Design, synthesis, and biological evaluation of Mannich bases of heterocyclic chalcone analogs as cytotoxic agents
    M Vijaya Bhaskar Reddy
    Department of Chemistry, National Cheng Kung University, Tainan 701, Taiwan
    Bioorg Med Chem 16:7358-70. 2008
    ..Out of the 39 chalcones synthesized, 31 compounds showed potent activity against at least one cell line with IC(50) values ranging from 0.03 to 3.80 microg/mL. Structure-activity relationships (SAR) are also discussed...
  99. pmc Synthesis of unsymmetrical biphenyls as potent cytotoxic agents
    Gang Wu
    Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China
    Bioorg Med Chem Lett 18:5272-6. 2008
    ....