inhibitory concentration 50

Summary

Summary: The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture.

Top Publications

  1. pmc Artemisinin resistance in Plasmodium falciparum malaria
    Arjen M Dondorp
    Mahidol Oxford Research Unit, Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand
    N Engl J Med 361:455-67. 2009
  2. pmc Decreasing pfmdr1 copy number in plasmodium falciparum malaria heightens susceptibility to mefloquine, lumefantrine, halofantrine, quinine, and artemisinin
    Amar bir Singh Sidhu
    Department of Microbiology and Immunology, Albert Einstein College of Medicine, Bronx, New York, Bronx, NY 10461, USA
    J Infect Dis 194:528-35. 2006
  3. pmc Decreased in vitro susceptibility of Plasmodium falciparum isolates to artesunate, mefloquine, chloroquine, and quinine in Cambodia from 2001 to 2007
    Pharath Lim
    Institut Pasteur in Cambodia, Molecular Epidemiology Unit, Phnom Penh, Cambodia
    Antimicrob Agents Chemother 54:2135-42. 2010
  4. ncbi Online analysis of in vitro resistance to antimalarial drugs through nonlinear regression
    Hervé Le Nagard
    INSERM Université Paris Diderot UMR 738, Paris, France
    Comput Methods Programs Biomed 104:10-8. 2011
  5. ncbi Effect of the lysophospholipid analogues edelfosine, ilmofosine and miltefosine against Leishmania amazonensis
    Ricardo M Santa-Rita
    Dept de Ultra estrutura e Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, 21045 900, Rio de Janeiro RJ, Brazil
    J Antimicrob Chemother 54:704-10. 2004
  6. ncbi A specific mechanism of nonspecific inhibition
    Susan L McGovern
    Department of Molecular Pharmacology and Biological Chemistry, Northwestern University, 303 East Chicago Avenue, Chicago, Illinois 60611, USA
    J Med Chem 46:4265-72. 2003
  7. pmc Pfmdr1 copy number and arteminisin derivatives combination therapy failure in falciparum malaria in Cambodia
    Pharath Lim
    Institut Pasteur in Cambodia, Phnom Penh, Cambodia
    Malar J 8:11. 2009
  8. ncbi Sterol methenyl transferase inhibitors alter the ultrastructure and function of the Leishmania amazonensis mitochondrion leading to potent growth inhibition
    Juliany C F Rodrigues
    Laboratorio de Ultraestrutura Celular Hertha Meyer, Instituto de Biofisica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, CCS Bloco G, Ilha do Fundao, 21949 900 Rio de Janeiro RJ, Brazil
    Protist 158:447-56. 2007
  9. pmc Reduced in vitro susceptibility to artemisinin derivatives associated with multi-resistance in a traveller returning from South-East Asia
    Bruno Pradines
    Unité de Recherche en Biologie et Epidémiologie Parasitaires Unité de Recherche pour les Maladies Infectieuses et Tropicales Emergentes UMR 6236, Institut de Medecine Tropicale du Service de Sante des Armees, Marseille, France
    Malar J 10:268. 2011
  10. pmc Effect of elatol, isolated from red seaweed Laurencia dendroidea, on Leishmania amazonensis
    Adriana Oliveira dos Santos
    Programa de Pós Graduação em Microbiologia, Universidade Estadual de Londrina, Rodovia Celso Garcia Cid, PR 445, Km 380, CEP 86051 990, Campus Universitario, Londrina, Parana, Brazil
    Mar Drugs 8:2733-43. 2010

Research Grants

  1. DRUG SUSCEPTIBILITY ASSAY FOR HCMV CLINICAL ISOLATES
    ROBYN MCGUIRE; Fiscal Year: 1999
  2. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2008
  3. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
  4. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
  5. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002
  6. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2004
  7. GARLIC PREPARATIONS AND ANTIRETROVIRAL DRUGS
    David Greenblatt; Fiscal Year: 2004
  8. HAART Regimens in Substance Abusers
    David Greenblatt; Fiscal Year: 2003
  9. DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORS
    Arun K Ghosh; Fiscal Year: 2010
  10. DEVELOPMENT OF LIGAND ASSISTED ASYMMETRIC SYNTHESES
    Arun Ghosh; Fiscal Year: 2001

Detail Information

Publications288 found, 100 shown here

  1. pmc Artemisinin resistance in Plasmodium falciparum malaria
    Arjen M Dondorp
    Mahidol Oxford Research Unit, Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand
    N Engl J Med 361:455-67. 2009
    ..There are recent concerns that the efficacy of such therapies has declined on the Thai-Cambodian border, historically a site of emerging antimalarial-drug resistance...
  2. pmc Decreasing pfmdr1 copy number in plasmodium falciparum malaria heightens susceptibility to mefloquine, lumefantrine, halofantrine, quinine, and artemisinin
    Amar bir Singh Sidhu
    Department of Microbiology and Immunology, Albert Einstein College of Medicine, Bronx, New York, Bronx, NY 10461, USA
    J Infect Dis 194:528-35. 2006
    ..These results highlight the importance of pfmdr1 copy number in determining P. falciparum susceptibility to multiple agents currently being used to combat malaria caused by multidrug-resistant parasites...
  3. pmc Decreased in vitro susceptibility of Plasmodium falciparum isolates to artesunate, mefloquine, chloroquine, and quinine in Cambodia from 2001 to 2007
    Pharath Lim
    Institut Pasteur in Cambodia, Molecular Epidemiology Unit, Phnom Penh, Cambodia
    Antimicrob Agents Chemother 54:2135-42. 2010
    ..These results are worrisome, because they may signal deterioration of the efficacy of artesunate-mefloquine beyond the Cambodian-Thai border...
  4. ncbi Online analysis of in vitro resistance to antimalarial drugs through nonlinear regression
    Hervé Le Nagard
    INSERM Université Paris Diderot UMR 738, Paris, France
    Comput Methods Programs Biomed 104:10-8. 2011
    ..This website is used by various teams in the world and the user can do the analysis without knowing R using the GUI. This article describes version 2.1 of this website and shows illustration on five different real examples...
  5. ncbi Effect of the lysophospholipid analogues edelfosine, ilmofosine and miltefosine against Leishmania amazonensis
    Ricardo M Santa-Rita
    Dept de Ultra estrutura e Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, 21045 900, Rio de Janeiro RJ, Brazil
    J Antimicrob Chemother 54:704-10. 2004
    ..Analysis of the effect of edelfosine, ilmofosine and miltefosine on Leishmania amazonensis and of potential targets of these lysophospholipid analogues...
  6. ncbi A specific mechanism of nonspecific inhibition
    Susan L McGovern
    Department of Molecular Pharmacology and Biological Chemistry, Northwestern University, 303 East Chicago Avenue, Chicago, Illinois 60611, USA
    J Med Chem 46:4265-72. 2003
    ..They also suggest a simple method to identify or reverse the action of aggregate-based inhibitors, which appear to be widespread...
  7. pmc Pfmdr1 copy number and arteminisin derivatives combination therapy failure in falciparum malaria in Cambodia
    Pharath Lim
    Institut Pasteur in Cambodia, Phnom Penh, Cambodia
    Malar J 8:11. 2009
    ....
  8. ncbi Sterol methenyl transferase inhibitors alter the ultrastructure and function of the Leishmania amazonensis mitochondrion leading to potent growth inhibition
    Juliany C F Rodrigues
    Laboratorio de Ultraestrutura Celular Hertha Meyer, Instituto de Biofisica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, CCS Bloco G, Ilha do Fundao, 21949 900 Rio de Janeiro RJ, Brazil
    Protist 158:447-56. 2007
    ..The present study confirms these findings, showing that in Leishmania amazonensis the mitochondrial complex appears to be the first organelle affected after treatment with different SMTI...
  9. pmc Reduced in vitro susceptibility to artemisinin derivatives associated with multi-resistance in a traveller returning from South-East Asia
    Bruno Pradines
    Unité de Recherche en Biologie et Epidémiologie Parasitaires Unité de Recherche pour les Maladies Infectieuses et Tropicales Emergentes UMR 6236, Institut de Medecine Tropicale du Service de Sante des Armees, Marseille, France
    Malar J 10:268. 2011
    ....
  10. pmc Effect of elatol, isolated from red seaweed Laurencia dendroidea, on Leishmania amazonensis
    Adriana Oliveira dos Santos
    Programa de Pós Graduação em Microbiologia, Universidade Estadual de Londrina, Rodovia Celso Garcia Cid, PR 445, Km 380, CEP 86051 990, Campus Universitario, Londrina, Parana, Brazil
    Mar Drugs 8:2733-43. 2010
    ..Our studies indicated that elatol is a potent antiproliferative agent against promastigote and intracellular amastigote forms, and may have important advantages for the development of new anti-leishamanial chemotherapies...
  11. pmc Plasmodium falciparum: development of a transgenic line for screening antimalarials using firefly luciferase as the reporter
    Long Cui
    Department of Entomology, The Pennsylvania State University, 501 ASI Building, University Park, PA 16802, USA
    Exp Parasitol 120:80-7. 2008
    ..Furthermore, the luciferase assay is robust with a Z' score of 0.77-0.92, which suggests the feasibility for further miniaturization and automation...
  12. pmc Dose-response curve slope sets class-specific limits on inhibitory potential of anti-HIV drugs
    Lin Shen
    Department of Medicine, Johns Hopkins University School of Medicine, 733 North Broadway, Baltimore, Maryland 21205, USA
    Nat Med 14:762-6. 2008
    ..Only agents with slopes >1 achieve high-level inhibition of single-round infectivity, a finding with profound implications for drug and vaccine development...
  13. ncbi Molecular analysis of pfatp6 and pfmdr1 polymorphisms and their association with in vitro sensitivity in Plasmodium falciparum isolates from the Thai-Myanmar border
    Papichaya Phompradit
    Thailand Center of Excellence on Drug Discovery and Development, Thammasat University, Rangsit Campus, Patumthani 12121, Thailand
    Acta Trop 120:130-5. 2011
    ..No association between mutation or amplification of pfatp6 gene and in vitro susceptibility of P. falciparum isolates was found...
  14. pmc Assessment of the drug susceptibility of Plasmodium falciparum clinical isolates from africa by using a Plasmodium lactate dehydrogenase immunodetection assay and an inhibitory maximum effect model for precise measurement of the 50-percent inhibitory conc
    Halima Kaddouri
    Centre National de Référence du Paludisme, Laboratoire de Parasitologie, Hôpital Bichat Claude Bernard and Université René Descartes, Paris, France
    Antimicrob Agents Chemother 50:3343-9. 2006
    ..The availability of this simple and highly sensitive pLDH immunodetection assay will provide an easier method for drug susceptibility testing of malaria parasites...
  15. pmc Novel marine phenazines as potential cancer chemopreventive and anti-inflammatory agents
    Tamara P Kondratyuk
    College of Pharmacy, University of Hawaii at Hilo, Hilo, HI 96720, USA
    Mar Drugs 10:451-64. 2012
    ..These data provide greater insight on the biological potential of phenazine derivatives, and some guidance on how various substituents may alter potential anti-inflammatory and anti-cancer effects...
  16. ncbi Butylated hydroxytoluene analogs: synthesis and evaluation of their multipotent antioxidant activities
    Wageeh A Yehye
    Department of Chemistry, Faculty of Science, University of Malaya, Kuala Lumpur 50603, Malaysia
    Molecules 17:7645-65. 2012
    ..Therefore, one can propose these new multipotent antioxidants (MPAOs) as potential antioxidants for tackling oxidative stress and lipid peroxidation processes...
  17. ncbi Antiprotozoal activities of traditional medicinal plants from the Garhwal region of North West Himalaya, India
    Virendra K Dua
    National Institute of Malaria Research, Field Unit, Hardwar 249403, India
    J Ethnopharmacol 136:123-8. 2011
    ....
  18. pmc A simple and inexpensive haemozoin-based colorimetric method to evaluate anti-malarial drug activity
    Tran Thanh Men
    Department of Biomolecular Engineering, Kyoto Institute of Technology, Matsugasaki, Sakyo ku, Kyoto 606 8585, Japan
    Malar J 11:272. 2012
    ..This study describes an inexpensive procedure that is based on the advantage of a positive correlation between the haemozoin level of infected erythrocytes and parasite load...
  19. pmc Combination therapy with gossypol reveals synergism against gemcitabine resistance in cancer cells with high BCL-2 expression
    Foong Ying Wong
    Department of Haematology Oncology, National University Health System, Singapore, Singapore
    PLoS ONE 7:e50786. 2012
    ....
  20. ncbi A novel triazolic naphthofuranquinone induces autophagy in reservosomes and impairment of mitosis in Trypanosoma cruzi
    M C Fernandes
    Laboratorio de Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ 21040 360, Brazil
    Parasitology 139:26-36. 2012
    ..TN could be a good starting point in the investigation of a chemotherapeutic approach for the treatment of Chagas' disease...
  21. pmc Comparison of a SYBR green I-based assay with a histidine-rich protein II enzyme-linked immunosorbent assay for in vitro antimalarial drug efficacy testing and application to clinical isolates
    David J Bacon
    Parasitology Program, Naval Medical Research Center Detachment, American Embassy, APO AA 34031, Lima, Peru
    Antimicrob Agents Chemother 51:1172-8. 2007
    ..falciparum with fresh or cultured parasites...
  22. ncbi Cytotoxic angucycline class glycosides from the deep sea actinomycete Streptomyces lusitanus SCSIO LR32
    Hongbo Huang
    Guangdong Key Laboratory of Marine Materia Medica, RNAM Center for Marine Microbiology, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, People s Republic of China
    J Nat Prod 75:202-8. 2012
    ..All compounds except grincamycin F (5) exhibited in vitro cytotoxicities against the human cancer cell lines HepG2, SW-1990, HeLa, NCI-H460, and MCF-7 and the mouse melanoma cell line B16, with IC₅₀ values ranging from 1.1 to 31 μM...
  23. pmc Antiprotozoal activities of organic extracts from French marine seaweeds
    Catherine Vonthron-Sénécheau
    Pharmacognosie et Molécules Naturelles Bio actives, Laboratoire d Innovation Thérapeutique UMR CNRS 7200, Faculte de Pharmacie, Universite de Strasbourg, 74 route du Rhin, 67401 Illkirch Cedex, France
    Mar Drugs 9:922-33. 2011
    ..falciparum, showed the best antiplasmodial activity. This study is the first to report comparative antiprotozoal activity of French marine algae. Some of the species studied here have not previously been biologically evaluated...
  24. ncbi The role of the 3D environment in hypoxia-induced drug and apoptosis resistance
    Jun W Kim
    UCLA Bioengineering, 5121 Engineering V, Los Angeles, CA 90095 1600, U S A
    Anticancer Res 31:3237-45. 2011
    ..The third dimension also brings mass transport into relevance, as inadequate diffusion of oxygen produces hypoxia. This study investigates the effects of distinct 3D environments on hypoxia-associated apoptosis and drug resistance...
  25. ncbi Antibiotics for prophylaxis of Plasmodium falciparum infections: in vitro activity of doxycycline against Senegalese isolates
    B Pradines
    , , Marseille, France
    Am J Trop Med Hyg 62:82-5. 2000
    ..falciparum to doxycycline and the other antimalarial drugs, and its original potential site of action are factors that favor its use as antimalarial drug...
  26. pmc Determinants of in vitro drug susceptibility testing of Plasmodium vivax
    B Russell
    International Health Program, Infectious Diseases Division, Menzies School of Health Research and Charles Darwin University, Darwin, Australia
    Antimicrob Agents Chemother 52:1040-5. 2008
    ..vivax and suggest that susceptibility to chloroquine may be associated with variable growth rates. These findings have important implications for the phenotypic and downstream genetic characterization of P. vivax...
  27. pmc Association of microsatellite variations of Plasmodium falciparum Na+/H+ exchanger (Pfnhe-1) gene with reduced in vitro susceptibility to quinine: lack of confirmation in clinical isolates from Africa
    Valérie Andriantsoanirina
    Institut Pasteur de Madagascar, Unité de Recherche sur le Paludisme, Antananarivo, Madagascar, France
    Am J Trop Med Hyg 82:782-7. 2010
    ..falciparum isolates from Africa. Because we did not include any isolate of Asian origin in our series, these results did not exclude the possibility of regional associations, for example in South-East Asia...
  28. ncbi Expression and function of pvcrt-o, a Plasmodium vivax ortholog of pfcrt, in Plasmodium falciparum and Dictyostelium discoideum
    Juliana Martha Sá
    Departamento de Parasitologia, Instituto de Ciencias Biomedicas, Universidade de Sao Paulo, Av Lineu Prestes 1374, Sao Paulo 05508 900, SP, Brazil
    Mol Biochem Parasitol 150:219-28. 2006
    ..Our data support an effect of PvCRT-o on chloroquine transport and/or accumulation by P. vivax, independent of the K76T amino acid substitution...
  29. ncbi Synthesis and antitumor properties of 2,5-bis(3'-indolyl)thiophenes: analogues of marine alkaloid nortopsentin
    Patrizia Diana
    Dipartimento Farmacochimico Tossicologico e Biologico, Universita degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy
    Bioorg Med Chem Lett 17:2342-6. 2007
    ....
  30. pmc Antiproliferative and cytostatic effects of the natural product eupatorin on MDA-MB-468 human breast cancer cells due to CYP1-mediated metabolism
    Vasilis Androutsopoulos
    Leicester School of Pharmacy, De Montfort University, The Gateway, Leicester, UK
    Breast Cancer Res 10:R39. 2008
    ..In this study, we aimed to identify a possible mechanism of action for the antiproliferative effect of eupatorin, which can be attributed to CYP1 family-mediated metabolism...
  31. pmc Reliability of antimalarial sensitivity tests depends on drug mechanisms of action
    Sharon Wein
    UMR 5235, Dynamique des Interactions Membranaires Normales et Pathologiques, CNRS Universite Montpellier II, Case 107, Place Eugene Bataillon, 34095 Montpellier, Cedex 05, France
    J Clin Microbiol 48:1651-60. 2010
    ..Some of them might not detect the antimalarial potential of new classes of compounds with innovative modes of action, which subsequently could become promising new antimalarial drugs...
  32. ncbi Potent and selective inhibitors of breast cancer resistance protein (ABCG2) derived from the p-glycoprotein (ABCB1) modulator tariquidar
    Matthias Kühnle
    Department of Pharmaceutical Medicinal Chemistry II, Institute of Pharmacy, Faculty of Chemistry and Pharmacy, University of Regensburg, D 93053 Regensburg, Germany
    J Med Chem 52:1190-7. 2009
    ..ABCG2 inhibitors might be useful for cancer treatment with respect to reversal of multidrug resistance, overcoming the BBB and targeting of tumor stem cells...
  33. pmc Trypanocidal activity of aziridinyl nitrobenzamide prodrugs
    Chris Bot
    Queen Mary Pre Clinical Drug Discovery Group, School of Biological and Chemical Sciences, Queen Mary University of London, London E1 4NS, United Kingdom
    Antimicrob Agents Chemother 54:4246-52. 2010
    ..We conclude that members of the aziridinyl nitrobenzamide class of nitroheterocycles provide new lead structures that have the potential to treat trypanosomal infections...
  34. ncbi Synthesis of a small library of 2-phenoxy-1,4-naphthoquinone and 2-phenoxy-1,4-anthraquinone derivatives bearing anti-trypanosomal and anti-leishmanial activity
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, Bologna University, Via Belmeloro 6, I 40126 Bologna, Italy
    Bioorg Med Chem Lett 18:2272-6. 2008
    ..28microM, and IC(50)=1.26microM, respectively)...
  35. ncbi Anti-hepatitis B virus activity of chlorogenic acid, quinic acid and caffeic acid in vivo and in vitro
    Gui Feng Wang
    Laboratory of Immunopharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, People s Republic of China
    Antiviral Res 83:186-90. 2009
    ..Both the extracts of regular coffee and that of decaffeinated coffee showed inhibitory effect on HBV replication...
  36. ncbi Anti-trypanosomal activity of helenalin and some structurally related sesquiterpene lactones
    Thomas J Schmidt
    Institut für Pharmazeutische Biologie der Heinrich Heine Universität, Dusseldorf, Germany
    Planta Med 68:750-1. 2002
    ..051 and 0.695 microM against T. brucei rhodesiense and T. cruzi, respectively. The low IC50 value for T. b. rhodesiense indicates that helenalin type compounds may be interesting candidates for further evaluation...
  37. ncbi Identification of species-specific determinants of the action of the antagonist capsazepine and the agonist PPAHV on TRPV1
    Elsa Phillips
    Novartis Institutes of Biomedical Research, Novartis Institute for Medical Sciences, 5 Gower Place, London WC1E 6BN, United Kingdom
    J Biol Chem 279:17165-72. 2004
    ..The rat M547L mutation reduced the affinity of RTX binding. Thus, amino acids within the S2-S4 region are important sites of agonist and antagonist interaction with TRPV1...
  38. pmc Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT
    Patrice Dubreuil
    INSERM, U891, Centre de Recherche en Cancerologie de Marseille, Signalisation, Hematopoiesis and Mechanisms of Oncogenesis, centre de référence des mastocytoses, Marseille, France
    PLoS ONE 4:e7258. 2009
    ..Here, we characterise the in vitro and in vivo profiles of masitinib (AB1010), a novel phenylaminothiazole-type tyrosine kinase inhibitor that targets KIT...
  39. ncbi A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors
    Adeela Kamal
    Conforma Therapeutics Corporation, 9393 Towne Centre Drive, Suite 240, San Diego, California 92121, USA
    Nature 425:407-10. 2003
    ..These results suggest that tumour cells contain Hsp90 complexes in an activated, high-affinity conformation that facilitates malignant progression, and that may represent a unique target for cancer therapeutics...
  40. pmc Increased tolerance to artemisinin in Plasmodium falciparum is mediated by a quiescence mechanism
    Benoit Witkowski
    CNRS, Laboratoire de Chimie de Coordination, UPR8241, Toulouse, France
    Antimicrob Agents Chemother 54:1872-7. 2010
    ....
  41. ncbi In vitro chemopreventive potential of fucophlorethols from the brown alga Fucus vesiculosus L. by anti-oxidant activity and inhibition of selected cytochrome P450 enzymes
    Sabine Parys
    Institute for Pharmaceutical Biology, University of Bonn, Nussallee 6, D 53115 Bonn, Germany
    Phytochemistry 71:221-9. 2010
    ..In addition, the compounds were shown to inhibit cytochrome P450 1A activity with IC(50) values in the range of 17.9-33 microg/ml, and aromatase (Cyp19) activity with IC(50) values in the range of 1.2-5.6 microg/ml...
  42. 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...
  43. ncbi Binding of ceftaroline to penicillin-binding proteins of Staphylococcus aureus and Streptococcus pneumoniae
    Helene Moisan
    Centre d étude et de valorisation de la diversité microbienne, Departement de Biologie, Universite de Sherbrooke, Sherbrooke, QC, Canada J1K 2R1
    J Antimicrob Chemother 65:713-6. 2010
    ..Ceftaroline is currently in Phase 3 development for the treatment of complicated skin and skin structure infections and community-acquired pneumonia, including infections caused by MRSA and multidrug-resistant S. pneumoniae...
  44. ncbi Phenotypic and structural analyses of hepatitis C virus NS3 protease Arg155 variants: sensitivity to telaprevir (VX-950) and interferon alpha
    Yi Zhou
    Vertex Pharmaceuticals Inc, Cambridge, Massachusetts 02139, USA
    J Biol Chem 282:22619-28. 2007
    ..Finally, these variant replicons were shown to have reduced replication capacity compared with the wild-type HCV replicon in cells...
  45. ncbi In vitro anti-trypanosomal activity of elatol isolated from red seaweed Laurencia dendroidea
    P Veiga-Santos
    Programa de Pós Graduação em Ciências Farmacêuticas, Laboratório de Inovação Tecnológica no Desenvolvimento de Fármacos e Cosméticos, Bloco B 08, Universidade Estadual de Maringa, Av Colombo 5790, CEP 87020 900 Maringa, Parana, Brazil
    Parasitology 137:1661-70. 2010
    ..This is the first report of the anti-trypanosomal effect of the sesquiterpene elatol...
  46. ncbi Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure
    Carsten Jagusch
    Pharmaceutical and Medicinal Chemistry, Saarland University, PO Box 151150, D 66041 Saarbrucken, Germany
    Bioorg Med Chem 16:1992-2010. 2008
    ..5 h vs 1.6 h). Docking studies revealed two new binding modes different from the one of the substrates and steroidal inhibitors...
  47. ncbi Molecular interactions of CCR5 with major classes of small-molecule anti-HIV CCR5 antagonists
    Rama Kondru
    Department of Medicinal Chemistry, Roche Palo Alto, 3431 Hillview Avenue, Palo Alto, CA 94304, USA
    Mol Pharmacol 73:789-800. 2008
    ..The fully mapped binding pocket of CCR5 is being used for structure-based design and lead optimization of novel anti-HIV CCR5 inhibitors with improved potency and better resistance profile...
  48. ncbi 3,4-Diaryl-isoxazoles and -imidazoles as potent dual inhibitors of p38alpha mitogen activated protein kinase and casein kinase 1delta
    Christian Peifer
    Department of Pharmacy, Eberhard Karls University, Auf der Morgenstelle 8, D 72076 Tuebingen, Germany
    J Med Chem 52:7618-30. 2009
    ..447 microM) possessing differentiated specificity. Selected compounds were profiled over 76 kinases and evaluation of their cellular efficacy showed 18 (CKP138) to be a highly potent and dual-specific inhibitor of CK1delta and p38alpha...
  49. pmc Artesunate misuse and Plasmodium falciparum malaria in traveler returning from Africa
    Dea Shahinas
    University of Toronto, Toronto, Ontario, Canada
    Emerg Infect Dis 16:1608-10. 2010
    ..Isolates had an elevated 50% inhibitory concentration to artemisinin, artesunate, and artemether, compared with that of other African isolates. Inappropriate use of artemisinin derivatives can reduce P. falciparum susceptibility...
  50. pmc Fexinidazole--a new oral nitroimidazole drug candidate entering clinical development for the treatment of sleeping sickness
    Els Torreele
    Drugs for Neglected Diseases Initiative DNDi, Geneva, Switzerland
    PLoS Negl Trop Dis 4:e923. 2010
    ..To complete the preclinical development and meet the regulatory requirements before initiating human trials, the anti-parasitic properties and the pharmacokinetic, metabolic and toxicological profile of fexinidazole have been assessed...
  51. pmc Failure of artesunate-mefloquine combination therapy for uncomplicated Plasmodium falciparum malaria in southern Cambodia
    William O Rogers
    Naval Medical Research Unit 2, Komp, P2P PLP LITBANGKES, Jl, Percetakan Negara No, 29, Jakarta 10560, Indonesia
    Malar J 8:10. 2009
    ..The efficacy of standard therapies for uncomplicated Plasmodium falciparum and Plasmodium vivax malaria was assessed in Chumkiri, Kampot Province, Cambodia...
  52. ncbi Bioactive novel polyphenols from the fruit of Manilkara zapota (Sapodilla)
    Jun Ma
    Department of Biological Sciences, Lehman College and The Graduate Center, The City University of New York, 250 Bedford Park Boulevard West, Bronx, New York 10468, USA
    J Nat Prod 66:983-6. 2003
    ..Compound 2 showed high antioxidant activity (IC(50) = 23.5 microM) in the DPPH free-radical assay and displayed cytotoxicity in the HCT-116 and SW-480 human colon cancer cell lines with IC(50) values of 154 and 134 microM, respectively...
  53. pmc In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax
    R N Price
    Global Health Division, Menzies School of Health Research, Charles Darwin University, Darwin, Australia
    Antimicrob Agents Chemother 54:5146-50. 2010
    ..vivax and P. falciparum highlights the suitability of the drug as a novel partner for artemisinin-based combination therapy in regions where the two species are coendemic...
  54. pmc In vitro activity of antifolate and polymorphism in dihydrofolate reductase of Plasmodium falciparum isolates from the Kenyan coast: emergence of parasites with Ile-164-Leu mutation
    Steven M Kiara
    Kenya Medical Research Institute KEMRI Wellcome Trust Collaborative Research Program, P O Box 230, 80108 Kilifi, Kenya
    Antimicrob Agents Chemother 53:3793-8. 2009
    ..We confirmed the presence of this mutation by sequencing. Thus, TMX and MTX are potent against P. falciparum, and quadruple mutants are now emerging in Africa...
  55. pmc In vitro and in vivo high-throughput assays for the testing of anti-Trypanosoma cruzi compounds
    Adriana M C Canavaci
    Center for Tropical and Emerging Global Diseases, University of Georgia, Athens, Georgia, United States of America
    PLoS Negl Trop Dis 4:e740. 2010
    ..With scant economic resources available for antiparasitic drug discovery and development, inexpensive, high-throughput and in vivo assays to screen potential new drugs and existing compound libraries are essential...
  56. pmc Atorvastatin as a potential anti-malarial drug: in vitro synergy in combinational therapy with quinine against Plasmodium falciparum
    Véronique Parquet
    Unité de Recherche en Biologie et Epidémiologie Parasitaires Unité de Recherche pour les Maladies Infectieuses et Tropicales Emergentes UMR 6236, Institut de Medecine Tropicale du Service de Sante des Armees, Marseille, France
    Malar J 9:139. 2010
    ....
  57. pmc Novel inhibitors of influenza virus fusion: structure-activity relationship and interaction with the viral hemagglutinin
    Evelien Vanderlinden
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    J Virol 84:4277-88. 2010
    ..Our studies with the new fusion inhibitor 4c confirm the importance of this HA region in the development of influenza virus fusion inhibitors...
  58. pmc A novel facile method of labeling octreotide with (18)F-fluorine
    Peter Laverman
    Department of Nuclear Medicine, Radboud University Nijmegen Medical Centre, Nijmegen, The Netherlands
    J Nucl Med 51:454-61. 2010
    ..The method is characterized by the labeling of NOTA-octreotide (NOTA-d-Phe-cyclo[Cys-Phe-d-Trp-Lys-Thr-Cys]-Throl (MH(+) 1305) [IMP466]) with (18)F...
  59. ncbi Lactoferrin inhibits enterovirus 71 infection of human embryonal rhabdomyosarcoma cells in vitro
    Tzou Yien Lin
    Department of Pediatrics, Chang Gung Children s Hospital, 5 Fu Hsin Street, Kweishan 333, Taoyuan, Taiwan
    J Infect Dis 186:1161-4. 2002
    ..5-24.5 microg/mL and 103.3-185.0 microg/mL, respectively). Lactoferrin probably exerts its effect at the level of viral adsorption, since the ongoing infection could not be further inhibited after the EV71 penetrated RD cells...
  60. pmc Gossypol induces apoptosis by activating p53 in prostate cancer cells and prostate tumor-initiating cells
    Suresh R Volate
    Cancer Stem Cell Section, Laboratory of Cancer Prevention, Center for Cancer Research, National Cancer Institute at Frederick, NIH, Frederick, Maryland 21702, USA
    Mol Cancer Ther 9:461-70. 2010
    ..These studies show for the first time that gossypol treatment induces DNA damage and activates p53. Collectively, these data support the use of gossypol as a novel agent for prostate cancer...
  61. ncbi The power issue: determination of KB or Ki from IC50. A closer look at the Cheng-Prusoff equation, the Schild plot and related power equations
    H C Cheng
    Safety Pharmacology, Drug Safety Evaluation, Aventis Pharmaceuticals Inc, Bridgewater, NJ 08807, USA
    J Pharmacol Toxicol Methods 46:61-71. 2001
    ..The purpose of this study is to illustrate that the slope function (K) of an agonist concentration-response curve is critical to the determination of KB values...
  62. pmc Species-specific pharmacology of Trichloro(sulfanyl)ethyl benzamides as transient receptor potential ankyrin 1 (TRPA1) antagonists
    Lana Klionsky
    Department of Neuroscience, Amgen, Inc, Thousand Oaks, California, USA
    Mol Pain 3:39. 2007
    ..In summary, we conclude that both human and rat TRPA1 channels show similar AITC and noxious cold activation profiles, but TCEB compounds display species-specific differential pharmacology at TRPA1...
  63. pmc Pyrimethamine and WR99210 exert opposing selection on dihydrofolate reductase from Plasmodium vivax
    Michele D Hastings
    Department of Genome Sciences, University of Washington, Box 357730, Seattle, WA 98195 7730
    Proc Natl Acad Sci U S A 99:13137-41. 2002
    ..If that is the case, this novel class of DHFR inhibitors could provide effective and affordable treatment for chloroquine- and pyrimethamine-resistant vivax and falciparum malaria for many years to come...
  64. ncbi Evaluation of combination chemotherapy: integration of nonlinear regression, curve shift, isobologram, and combination index analyses
    Liang Zhao
    College of Pharmacy and James Cancer Hospital and Solove Research Institute, The Ohio State University, Columbus, OH 43210, USA
    Clin Cancer Res 10:7994-8004. 2004
    ....
  65. ncbi Sensitivity to antifolates and genetic analysis of Plasmodium vivax isolates from Thailand
    Kanchana Rungsihirunrat
    Faculty of Allied Health Sciences, Thammasat University, Pathumtani, Thailand
    Am J Trop Med Hyg 76:1057-65. 2007
    ..Results suggest that quadruple mutant alleles confer decreased sensitivity to pyrimethamine but retain sensitivity to WR99210...
  66. pmc In vitro susceptibilities of Leishmania donovani promastigote and amastigote stages to antileishmanial reference drugs: practical relevance of stage-specific differences
    Marieke Vermeersch
    Laboratory for Microbiology, Parasitology, and Hygiene LMPH, Faculty of Pharmaceutical, Biomedical, and Veterinary Sciences, University of Antwerp, Groenenborgerlaan 171, 2020 Antwerp, Belgium
    Antimicrob Agents Chemother 53:3855-9. 2009
    ..Axenic systems can be recommended only for compounds for which no cellular mechanisms are involved, for example, amphotericin B and miltefosine...
  67. pmc Inhibitory activity of marine sponge-derived natural products against parasitic protozoa
    Ilkay Orhan
    Department of Pharmacognosy, Faculty of Pharmacy, Gazi University, TR 06330 Ankara, Turkey
    Mar Drugs 8:47-58. 2010
    ..This is the first report of antiprotozoal activity of marine metabolites 1-14, and points out the potential of marine sponges in discovery of new antiprotozoal lead compounds...
  68. ncbi Lobophorins E and F, new spirotetronate antibiotics from a South China Sea-derived Streptomyces sp. SCSIO 01127
    Siwen Niu
    CAS Key Laboratory of Marine Bio resources Sustainable Utilization, RNAM Center for Marine Microbiology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou, PR China
    J Antibiot (Tokyo) 64:711-6. 2011
    ..Lobophorin F (2) also displayed better cytotoxic activities than lobophorin B (4), with IC(50) of 6.82, 2.93 and 3.16 μM against SF-268, MCF-7 and NCI-H460, respectively...
  69. pmc Plasmodium falciparum resistance to cytocidal versus cytostatic effects of chloroquine
    Michelle F Paguio
    Department of Chemistry, Georgetown University, Washington, DC 20057, United States
    Mol Biochem Parasitol 178:1-6. 2011
    ..falciparum. The results have important implications for development of new antimalarial drugs and for fully defining the genetic loci that confer clinically relevant antimalarial drug resistance phenomena...
  70. ncbi Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors
    Craig W Lindsley
    Department of Medicinal Chemistry, Technology Enabled Synthesis Group, Merck Research Laboratories, Merck and Co, PO Box 4, West Point, PA 19486, USA
    Bioorg Med Chem Lett 15:761-4. 2005
    ..An iterative analog library synthesis approach quickly provided a highly selective Akt1/Akt2 inhibitor that induces apoptosis in tumor cells and inhibits Akt phosphorylation in vivo...
  71. pmc Arenamides A-C, cytotoxic NFkappaB inhibitors from the marine actinomycete Salinispora arenicola
    Ratnakar N Asolkar
    Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California, San Diego, La Jolla, California 92093 0204, USA
    J Nat Prod 72:396-402. 2009
    ..Taken together, these data suggest that the chemoprevention and anti-inflammatory characteristics of arenamides A and B warrant further investigation...
  72. ncbi Antimycobacterial, antiprotozoal and cytotoxic potential of twenty-one brown algae (Phaeophyceae) from British and Irish waters
    Jasmine Spavieri
    Department of Pharmaceutical and Biological Chemistry, Centre for Pharmacognosy and Phytotherapy, School of Pharmacy, University of London, London WC1N 1AX, UK
    Phytother Res 24:1724-9. 2010
    ..e. H. siliquosa, B. bifurcata and Cystoseira tamariscifolia showed some cytotoxicity. To our knowledge, this is the first study on the antiprotozoal and antimycobacterial activity of brown algae from British and Irish waters...
  73. ncbi Antileishmanial sesquiterpene lactones from Pseudelephantopus spicatus, a traditional remedy from the Chayahuita Amerindians (Peru). Part III
    G Odonne
    CNRS UMR Ecofog, Universite des Antilles et de la Guyane, BP792, 97337 Cayenne cedex, France
    J Ethnopharmacol 137:875-9. 2011
    ..ex Aubl.) C.F. Baker, which has demonstrated strong biological activity towards Leishmania amazonensis. Our goal was to discover the active compound of this plant-based remedy...
  74. ncbi Cytotoxic bipyridines from the marine-derived actinomycete Actinoalloteichus cyanogriseus WH1-2216-6
    Peng Fu
    Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, People s Republic of China
    J Nat Prod 74:1751-6. 2011
    ..26 to 15.7 μM. Compounds 7 and 8 also showed antimicrobial activities against Escherichia coli, Aerobacter aerogenes, Pseudomonas aeruginosa, and Candida albicans, with MIC values of 9.7 to 38.6 μM...
  75. ncbi Cytotoxic norsesquiterpene peroxides from the endophytic fungus Talaromyces flavus isolated from the mangrove plant Sonneratia apetala
    Hanxiang Li
    School of Chemistry and Chemical Engineering, Sun Yat Sen University, Guangzhou 510275, People s Republic of China
    J Nat Prod 74:1230-5. 2011
    ..Compounds 2 and 4 showed cytotoxicity against the five human cancer cell lines with IC50 values between 0.70 and 2.78 μg/mL...
  76. ncbi Growth of ligand-target interaction data in ChEMBL is associated with increasing and activity measurement-dependent compound promiscuity
    Ye Hu
    Department of Life Science Informatics, B IT, LIMES Program Unit Chemical Biology and Medicinal Chemistry, Rheinische Friedrich Wilhelms Universitat, Dahlmannstr 2, D 53113 Bonn, Germany
    J Chem Inf Model 52:2550-8. 2012
    ....
  77. pmc Ex vivo drug sensitivity profiles of Plasmodium falciparum field isolates from Cambodia and Thailand, 2005 to 2010, determined by a histidine-rich protein-2 assay
    Stuart D Tyner
    Department of Immunology and Medicine, US Army Medical Corps, Armed Forces Research Institute of Medical Sciences, Bangkok, Thailand
    Malar J 11:198. 2012
    ....
  78. ncbi QSAR study on 5-lipoxygenase inhibitors based on support vector machine
    Bing Niu
    College of Life Science, Shanghai University, Shanghai 200444, China
    Med Chem 8:1108-16. 2012
    ..An online web server for activity prediction is available at http://chemdata.shu.edu.cn/qsar5lip...
  79. ncbi Discovery, characterization, and structure-activity relationships studies of proapoptotic polyphenols targeting B-cell lymphocyte/leukemia-2 proteins
    Shinichi Kitada
    The Burnham Institute, 10901 North Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 46:4259-64. 2003
    ....
  80. pmc AT-406, an orally active antagonist of multiple inhibitor of apoptosis proteins, inhibits progression of human ovarian cancer
    Melissa K Brunckhorst
    Department of Oncological Sciences, Mount Sinai School of Medicine, New York, NY, USA
    Cancer Biol Ther 13:804-11. 2012
    ....
  81. ncbi Discovery and preliminary structure-activity relationship analysis of 1,14-sperminediphenylacetamides as potent and selective antimalarial lead compounds
    Lydia P P Liew
    School of Chemical Sciences, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand
    Bioorg Med Chem Lett 23:452-4. 2013
    ..falciparum makes this compound class of interest in the development of new antimalarial therapeutics...
  82. pmc Optimizing the HRP-2 in vitro malaria drug susceptibility assay using a reference clone to improve comparisons of Plasmodium falciparum field isolates
    Wiriya Rutvisuttinunt
    Department of Immunology and Medicine, US Army Medical Corps, Armed Forces Research Institute of Medical Sciences USAMC AFRIMS, Bangkok, Thailand
    Malar J 11:325. 2012
    ..Although in vitro anti-malarial susceptibility tests are widely used, uncertainties remain regarding interpretation of P. falciparum field isolate values...
  83. pmc Ribonuclease inhibitor as an intracellular sentry
    Marcia C Haigis
    Department of Biochemistry, University of Wisconsin Madison, Madison, WI 53706 1544, USA
    Nucleic Acids Res 31:1024-32. 2003
    ..Thus, RI constrains the cytotoxicity of RNase A. These data provide new insights for the development of an optimal ribonuclease-based cancer chemotherapy...
  84. pmc Synthesis and antimalarial and antituberculosis activities of a series of natural and unnatural 4-methoxy-6-styryl-pyran-2-ones, dihydro analogues and photo-dimers
    Stephen T McCracken
    School of Chemical Sciences, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand
    Bioorg Med Chem 20:1482-93. 2012
    ..donovani (IC(50) 4.5 μM), suggesting further elaboration of this latter scaffold could lead to the identification of new leads for the dual treatment of malaria and leishmaniasis...
  85. ncbi New diketopiperazine derivatives from a deep-sea-derived Nocardiopsis alba SCSIO 03039
    Qingbo Zhang
    CAS Key Laboratory of Marine Bio resources Sustainable Utilization, RNAM Center for Marine Microbiology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou, China
    J Antibiot (Tokyo) 66:31-6. 2013
    ..0 and 20.6 μM). The other compounds showed less pronounced cytotoxities against three tested human cancer cell lines and no compounds displayed antibacterial activities toward four indicator strains...
  86. ncbi Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors
    Qingzhong Hu
    Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D 66123 Saarbrucken, Germany
    J Med Chem 53:5049-53. 2010
    ....
  87. ncbi Oregano: chemical analysis and evaluation of its antimalarial, antioxidant, and cytotoxic activities
    Fatiha El Babili
    Faculté des Sciences Pharmaceutiques de Toulouse, Laboratoire de Botanique Mycologie, 35 ch des Maraîchers, F 31062 Toulouse, France
    J Food Sci 76:C512-8. 2011
    ..In addition, ethyl acetate extract (30 mg/L) and ethanol extract (56 mg/L) showed activity against human breast cancer cells (MCF7). The oregano essential oil was considered to be nontoxic...
  88. ncbi Inhibitory effect of quercetin on matrix metalloproteinase 9 activity molecular mechanism and structure-activity relationship of the flavonoid-enzyme interaction
    Alejandra C Saragusti
    Centro de Investigaciones en Bioquímica Clínica e Inmunología CIBICI, Consejo Nacional de Investigaciones Cientificas y Tecnicas CONICET, Argentina
    Eur J Pharmacol 644:138-45. 2010
    ....
  89. pmc In vitro susceptibility to quinine and microsatellite variations of the Plasmodium falciparum Na+/H+ exchanger (Pfnhe-1) gene: the absence of association in clinical isolates from the Republic of Congo
    Sebastien Briolant
    Unite de Parasitologie, Unite Mixte de Recherche 6236, Institut de Recherche Biomédicale des Armées Antenne de Marseille, Marseille, France
    Malar J 10:37. 2011
    ..In the present study, association between Pfnhe and QNR is investigated in a series of isolates from central Africa...
  90. ncbi Evaluation of Turkish seaweeds for antiprotozoal, antimycobacterial and cytotoxic activities
    Sevda Süzgeç-Selçuk
    Department of Pharmacognosy, Faculty of Pharmacy, University of Istanbul, Istanbul, Turkey
    Phytother Res 25:778-83. 2011
    ..This is the second study investigating the antiprotozoal activities of Turkish marine algae and identifies Dasya pedicellata, an understudied algal species, as a candidate for further studies...
  91. ncbi 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...
  92. ncbi In vitro effects of the BH3 mimetic, (-)-gossypol, on head and neck squamous cell carcinoma cells
    Christopher L Oliver
    Department of Otolaryngology Head and Neck Surgery, University of Michigan, Ann Arbor, Michigan 48109 0312, USA
    Clin Cancer Res 10:7757-63. 2004
    ..Gossypol, the levorotatory isomer of a natural product isolated from cottonseeds and roots, was recently discovered to bind to the BH3 binding groove of Bcl-xL and Bcl-2...
  93. ncbi Protein kinases CK1 and CK2 as new targets for neurodegenerative diseases
    Daniel I Perez
    Instituto de Quimica Medica CSIC, Juan de la Cierva 3, 28006 Madrid, Spain
    Med Res Rev 31:924-54. 2011
    ..The role of these two kinases in the molecular pathology of different neurodegenerative diseases together with different chemical families that are able to more or less specifically inhibit CK1 and CK2 are discussed in this review...
  94. ncbi Development and optimization of a binding assay for the XIAP BIR3 domain using fluorescence polarization
    Zaneta Nikolovska-Coleska
    University of Michigan Comprehensive Cancer Center, Departments of Internal Medicine and Medicinal Chemistry, University of Michigan, 1500 E Medical Center Drive, Ann Arbor, MI 48109 0934, USA
    Anal Biochem 332:261-73. 2004
    ....
  95. ncbi Typhonium flagelliforme induces apoptosis in CEMss cells via activation of caspase-9, PARP cleavage and cytochrome c release: its activation coupled with G0/G1 phase cell cycle arrest
    Syam Mohan
    UPM MAKNA Cancer Research Laboratory, Institute of Bioscience, University Putra Malaysia, 43400 Serdang, Malaysia
    J Ethnopharmacol 131:592-600. 2010
    ..The plant Typhonium flagelliforme (TF), commonly known as 'rodent tuber' in Malaysia, is often used as traditional remedy for cancer, including leukemia...
  96. pmc Cytotoxic activity of Thai medicinal plants against human cholangiocarcinoma, laryngeal and hepatocarcinoma cells in vitro
    Wiratchanee Mahavorasirikul
    Graduate Program in Biomedical Sciences, Thammasat University Rangsit Campus, Pathumtani 12121, Thailand
    BMC Complement Altern Med 10:55. 2010
    ....
  97. ncbi Novel imidazol-1-ylmethyl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-ones as potent and selective CYP11B1 inhibitors for the treatment of Cushing's syndrome
    Lina Yin
    Pharmaceutical and Medicinal Chemistry, Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland HIPS, Campus C2 3, D 66123 Saarbrucken, Germany
    J Med Chem 55:6629-33. 2012
    ..2 nM) than leads and more selective (SF = 11) than I and metyrapone. Since it also showed potent inhibition of rat CYP11B1 and good selectivity over human CYP17 and CYP19, it is a promising candidate for further development...
  98. pmc Phenotypic and genotypic analysis of in vitro-selected artemisinin-resistant progeny of Plasmodium falciparum
    Matthew S Tucker
    Department of Global Health, College of Public Health, University of South Florida, Tampa, Florida, USA
    Antimicrob Agents Chemother 56:302-14. 2012
    ..In summary, we define the artemisinin resistance phenotype as a decrease in susceptibility to artemisinins along with the ability to recover from drug-induced dormancy following supraclinical concentrations of the drug...
  99. ncbi Induction of apoptosis and cell cycle arrest by a chalcone panduratin A isolated from Kaempferia pandurata in androgen-independent human prostate cancer cells PC3 and DU145
    Jung Mi Yun
    Department of Biotechnology, Yonsei University, Seoul 120 749, Korea
    Carcinogenesis 27:1454-64. 2006
    ..These findings suggest that panduratin A may be an effective chemopreventive or therapeutic agent against CaP...
  100. pmc A comparative study of a flow-cytometry-based assessment of in vitro Plasmodium falciparum drug sensitivity
    Stephan Karl
    School of Physics, M013, The University of Western Australia, 35 Stirling Highway, Crawley WA 6009, Australia
    Malar J 8:294. 2009
    ..falciparum lactate dehydrogenase assay, the tritiated hypoxanthine incorporation assay, a previously described Sybr Green based plate reader assay and light microscopy...
  101. pmc The Mediterranean red alga Asparagopsis: a source of compounds against Leishmania
    Giuseppa Genovese
    Department of Life Sciences M Malpighi Botany, University of Messina, Salita Sperone, 31, 98166 Messina, Italy
    Mar Drugs 7:361-6. 2009
    ..Extracts from both species revealed remarkable antiprotozoal activity against Leishmania, revealing such algae as a great source of natural antiprotozoal products...

Research Grants49

  1. DRUG SUSCEPTIBILITY ASSAY FOR HCMV CLINICAL ISOLATES
    ROBYN MCGUIRE; Fiscal Year: 1999
    ..positive cells in the presence of inhibitory concentrations of antiviral drugs is used to determine inhibitory concentration 50 (IC50) values...
  2. 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. ..
  3. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
    ..abstract_text> ..
  4. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
    ..abstract_text> ..
  5. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  6. 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. ..
  7. GARLIC PREPARATIONS AND ANTIRETROVIRAL DRUGS
    David Greenblatt; Fiscal Year: 2004
    ..The work will provide immediately applicable clinical data on garlic interactions with antiretrovirals, as well as mechanistic data identifying the interaction process and its predictability from in vitro models. ..
  8. HAART Regimens in Substance Abusers
    David Greenblatt; Fiscal Year: 2003
    ....
  9. DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORS
    Arun K Ghosh; Fiscal Year: 2010
    ..This research integrates organic synthesis, protein-ligand x-ray crystallography, molecular modeling and in-depth virus and cell-biological studies to design the next generation of HIV-1 protease inhibitors. ..
  10. DEVELOPMENT OF LIGAND ASSISTED ASYMMETRIC SYNTHESES
    Arun Ghosh; Fiscal Year: 2001
    ..Besides the broad range of scope and generality, this line of research will provide excellent opportunities to teach and train graduate and undergraduate students in the laboratory. ..
  11. CHRONIC BENZODIAZEPINES: BEHAVIOR AND NEUROCHEMISTRY
    David Greenblatt; Fiscal Year: 2005
    ....
  12. MDR1 and Related Proteins during HIV PI Exposure
    David Greenblatt; Fiscal Year: 2005
    ..The findings will be of importance in understanding lipid disorders related to PIs as well as the kinetics of drugs used to treat HIV and related disorders. ..
  13. CYP3A Function in Aging AfricanAmericans
    David Greenblatt; Fiscal Year: 2006
    ..This study should provide important mechanistic information on the role of age, gender, and ethnicity as sources of variability in CYP3A-mediated drug metabolism and response. ..
  14. ANTIRETROVIRAL THERAPIES AND SUBSTANCE ABUSE
    David Greenblatt; Fiscal Year: 2002
    ..The in vitro model, if validated, has the potential to provide clinically important information on interactions involving HIV treatments and abusable drugs, at relatively low cost and with no human drug exposure. ..
  15. Metabolic Consequences of HAART: CYP3A and P-gp
    David Greenblatt; Fiscal Year: 2003
    ..This multidisciplinary proposal provides a clinical and scientific basis to assess the effects of currently available as well as experimental HAART medications on human CYP3A and P-gp. ..
  16. Novel Therapeutics for Bacillus anthracis
    Michael Johnson; Fiscal Year: 2007
    ..A bioassay core will provide a variety of assays for identifying and evaluating lead therapeutic agents. An administrative core will provide fiscal management and administrative support. ..
  17. Small Molecule Alanine Racemase Inhibitors as Novel Therapeutics for Tuberculosis
    Karen Anthony; Fiscal Year: 2006
    ..About 50 million people are infected with TB bacteria that are not susceptible to available antibiotics. The goal of this research is to develop new antibiotics to treat drug-resistant TB. [unreadable] [unreadable] [unreadable]..
  18. Identification of Ebola Virus Entry Inhibitors
    Arnab Basu; Fiscal Year: 2007
    ..Prioritize screening hits based on spectrum, cytotoxicity and mechanism. The end result of Phase 1 work will be identification of hits specific for EBOV entry inhibition. [unreadable] [unreadable] [unreadable]..
  19. Differential Cytokine Secretion by Human Basophils
    John Schroeder; Fiscal Year: 2008
    ..Thus, these differential effects on basophil IL-4 and IL-13, mediated through TLR, may also help in delineating the mechanisms regulating cytokine production. ..
  20. Purchase of a 400 MHz Multi-Nuclear NMR Spectrometer
    JOSEPH RICE; Fiscal Year: 2008
    ..The availability of a high resolution multi-nuclear NMR spectrometer is an essential tool for determining the chemical structures of these compounds and advancing these research efforts. [unreadable] [unreadable] [unreadable]..
  21. Small Molecule West Nile Virus Inhibitors
    Karen Anthony; Fiscal Year: 2008
    ..There is no proven treatment available. This research will identify small molecule drugs to treat illness caused by WN virus infections in humans. [unreadable] [unreadable] [unreadable]..
  22. The 7th International Conference on Head and Neck Cancer
    Jeffrey Myers; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  23. ANTIFUNGALS FROM MARINE INVERTEBRATES--AIDS ADJUVANTS
    Tadeusz F Molinski; Fiscal Year: 2010
    ..Optimized leads identified from those libraries will be advanced to in vitro and in vivo trials. ..
  24. THE PHYSIOLOGY OF DRUG RESISTANT MALARIA
    PAUL ROEPE; Fiscal Year: 2009
    ..Knowledge gained during this research will significantly expand our understanding of malarial parasite physiology and antimalarial drug resistance. ..
  25. Nanoscale-Natural Products Chemistry
    TADEUSZ MOLINSKI; Fiscal Year: 2009
    ....
  26. SALIVARY PROTEINS IN DENTAL INTEGUMENTS
    FRANK OPPENHEIM; Fiscal Year: 2009
    ..abstract_text> ..
  27. Expression of Proapoptotic Genes for Cancer Therapy
    Bingliang Fang; Fiscal Year: 2006
    ..Success of the proposed studies will lead to new therapeutics for refractory metastatic disease. It will also provide insight into mechanisms of resistance to apoptosis induction in cancer cells. ..
  28. Cryptococcus gatti mating 1oci; mapping and gene study
    Vishnu Chaturvedi; Fiscal Year: 2004
    ..abstract_text> ..
  29. VACCINES ELICITING CD8 CYTOTOXIC T CELL RESPONSES
    Herman Eisen; Fiscal Year: 2002
    ....
  30. QUANTITATIVE CARCINOGENESIS IN CULTURED EPITHELIAL CELLS
    Molly Kulesz Martin; Fiscal Year: 2002
    ..Knowledge of different functional p53 protein forms in cells and cooperating factors may improve the resolution, prognosis or treatment plan for human tumors with selective loss of distinct p53 functions. ..
  31. Peptides/MHC-I complexes and CD8+T cells
    Herman Eisen; Fiscal Year: 2004
    ..The overall goal is to help provide a platform to aid in the development of immunization strategies leading to increased yields of potent memory CD8 T cells. ..
  32. NOVEL PROBES FOR IMMUNOPHILIN MEDIATED CELL CONTROL
    TADEUSZ MOLINSKI; Fiscal Year: 2001
    ..5. To understand how modulation of the FKBP12/ryanodine receptor complex by bastadins influences cellular growth and differentiation using the BC3H1 cell line as model. ..
  33. Natural Product Antitumor Inducers of Apoptosis
    TADEUSZ MOLINSKI; Fiscal Year: 2004
    ..abstract_text> ..
  34. Mechanisms of SPAF and AS-FGF-2 in malignant conversion
    Molly Kulesz Martin; Fiscal Year: 2005
    ..The characterization of this bi-directional gene may provide useful prognosis markers as well as new targets for cancer therapy. ..
  35. Identification of HCV E1 an E2 Inhibitors
    Arnab Basu; Fiscal Year: 2006
    ..The most promising compound will advance to IND-enabling toxicology and pharmacology studies in two species (Phase III). [unreadable] [unreadable]..
  36. ADRENAL NICOTINIC RECEPTORS AND CATECHOLAMINE SECRETION
    DENNIS MCKAY; Fiscal Year: 2001
    ..These studies should contribute significantly to our current knowledge of adrenal nAChRs and may also contribute to our basic understanding of neuronal nAChRs and their regulation. ..
  37. Novel Biological Activities of Anti-Viral Antibody
    Donald Forthal; Fiscal Year: 2006
    ..This project may provide crucial insights for guiding the development of vaccines, immunoprophylaxis and immunotherapy. ..
  38. In vitro substrate assay for multi-drug resistance
    DONALD MELCHIOR; Fiscal Year: 2005
    ..The Fluorosome-frans-pgp assay is adaptable to multiwell plate formats and robotics, for eventual moderate to high throughput screening of drug candidate libraries. ..
  39. Green Tea Targets COX-2/PGE2 and EFGR Pathways in NSCLC via Stimulating Annexin 1
    Qing Yi Lu; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  40. A Linkage Map for Schistosoma mansoni
    Tim Anderson; Fiscal Year: 2008
    ..Development of a linkage map will pave the way for finding these genes. [unreadable] [unreadable] [unreadable]..
  41. APPLICATION OF NOVEL OPTICAL METHODS TO CELL DYNAMICS
    Alan Verkman; Fiscal Year: 2006
    ..abstract_text> ..
  42. REDOX PHARMACOLOGY OF T CHANNELS IN DRG NEURONS
    SLOBODAN TODOROVIC; Fiscal Year: 2009
    ..In addition, our results suggest an unexplored avenue for the development of potential novel therapies for pain control. ..
  43. MULTIPLE CLASSES OF CA2+ CHANNELS - SENSORY TRANSMISSION
    SLOBODAN TODOROVIC; Fiscal Year: 2004
    ..abstract_text> ..
  44. COMBINATORIAL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    John Cashman; Fiscal Year: 2001
    ..The study will provide an understanding of the structural and pharmaceutical properties of hDAT antagonists. The work will lead to new insight into the preparation of human medications necessary in the cessation of cocaine abuse. ..
  45. New Opioids for Alcoholism
    John Cashman; Fiscal Year: 2006
    ..The potential commercial application of the work is that the research could lead to a 'blockbuster' drug product. [unreadable] [unreadable]..
  46. PHYSIOLOGY AND MOLECULAR BIOLOGY OF LUNG WATER TRANSPORT
    Alan Verkman; Fiscal Year: 2007
    ..abstract_text> ..
  47. Anesthetics block neuronal voltage-gated Ca2+ currents
    SLOBODAN TODOROVIC; Fiscal Year: 2009
    ..abstract_text> ..