Page last updated: 2024-08-21

alpha-naphthoflavone and ketoconazole

alpha-naphthoflavone has been researched along with ketoconazole in 62 studies

Research

Studies (62)

TimeframeStudies, this research(%)All Research%
pre-19901 (1.61)18.7374
1990's8 (12.90)18.2507
2000's11 (17.74)29.6817
2010's23 (37.10)24.3611
2020's19 (30.65)2.80

Authors

AuthorsStudies
Cole, PA; Robinson, CH1
Hashizume, H; Kawasaki, M; Komatsu, M; Matsumoto, M; Sasaki, H; Shimokawa, Y; Tomishige, T; Tsubouchi, H1
Atodiresei, I; Fiebig, HH; Fleischhauer, J; Gerhäuser, C; Kehraus, S; Klimo, K; König, GM; Krick, A; Maier, A; Nieger, M; Raabe, G1
Muftuoglu, Y; Mustata, G1
Amblard, F; Bobeck, DR; Coats, SJ; McBrayer, TR; Schinazi, RF; Shi, J; Tao, S; Tharnish, PM; Whitaker, T; Zhang, H; Zhou, L1
Amblard, F; Bobeck, DR; Chavre, S; Coats, SJ; McBrayer, TR; Nettles, JH; Schinazi, RF; Shi, J; Tharnish, P; Whitaker, T; Zhang, H; Zhou, L1
Bae, IH; Choi, JK; Chough, C; Jang, SK; Keum, SJ; Kim, BM; Kim, H1
Cheon, SH; Choi, K; Hahn, HG; Han, M; Song, C; Yun, J1
Hahn, HG; Han, M; Jeong, N; Song, C1
Aubé, J; Chu, YK; Chung, D; Golden, JE; Guo, H; Jonsson, CB; McKellip, S; Noah, JW; Rasmussen, L; Roy, S; Schroeder, CE; Smith, LH; Smith, RA; Sosa, M; Sotsky, J; Tower, NA; White, EL; Yao, T1
Kheylik, Y; Kondratov, I; Krasavin, M; Naumchyk, V; Platonov, M; Zahanich, I; Zozulya, S1
Carazo, A; Drechslerová, M; Hrušková, ZR; Hyrsova, L; Kuneš, J; Nova, A; Pavek, P; Pour, M; Smutny, T; Špulák, M1
Kovalenko, A; Krasavin, M; Lukin, A; Moore, D; Tikhonova, IG; Zahanich, I; Zhurilo, N; Zozulya, S1
Cheng, M; Hao, C; Liu, C; Su, X; Sun, B; Wei, P; Zhang, X; Zhao, D; Zhao, L; Zhao, S1
Edginton, AN; McEneny-King, A; Osman, W; Rao, PPN1
Cheng, M; Hao, C; Liu, C; Su, X; Wei, P; Wu, M; Zhang, X; Zhao, D; Zhao, L; Zhao, S1
Chen, F; Chen, W; Lan, L; Li, B; Li, J; Liu, Y; Mao, F; Ni, S; Wei, H; Zhu, J1
Eugster, HP; Hinnen, A; Meyer, UA; Sengstag, C; Würgler, FE1
Bickers, DR; Das, M; Kaufmann, I; Merk, HF; Mukhtar, H1
Dushkin, MI; Menshikova, EB; Pivovarova, EN; Volsky, NN; Zenkov, NK1
Coon, MJ; Ding, X1
Eugster, HP; Sengstag, C1
Sequeira, DJ; Strobel, HW1
Baune, B; Becquemont, L; Farinotti, R; Flinois, JP; Furlan, V; Gimenez, F; Taburet, AM1
Chiba, K; Kobayashi, K; Nakajima, M; Oshima, K; Shimada, N; Tokudome, S; Yokoi, T1
Fink-Gremmels, J; Kuilman, ME; Maas, RF1
Greenblatt, DJ; Hesse, LM; Shader, RI; Venkatakrishnan, K; von Moltke, LL1
Bigler, L; Follath, F; Ha, HR; Kozlik, P; Stieger, B1
Breskvar, K; Lenasi, H1
Cavret, S; Feidt, C1
Hao, K; Liu, XQ; Liu, YT; Wang, GJ1
Liu, XQ; Wang, GJ; Zhao, XP; Zhong, J1
Liu, ZH; Zeng, S1
Hu, JH; Qian, M; Shi, LF1
Greenhaw, J; Salminen, WF; Shi, Q; Yang, X1
Kubickova, B; Martinkova, M; Stiborova, M1
Greenhaw, J; Salminen, WF; Shi, Q1
Bryant, MS; Guo, L; Ning, B; Ren, Z; Wu, Q; Xuan, J1
Bao, QC; Jia, JM; Jiang, F; Jin, YH; Li, DD; Liu, F; Wang, HJ; Wang, L; Wang, ZH; Xu, XL; You, QD; Zhang, Q1
Cheng, M; Hao, C; Jiang, X; Su, X; Wei, P; Wu, M; Zhang, X; Zhao, D; Zhao, L; Zhao, S1
Cini, E; De Santis, R; Giannini, G; Manera, F; Manetti, F; Milazzo, FM; Pace, S; Petricci, E; Stasi, MA; Tallarico, C; Vesci, L1
Chen, CH; De Clercq, E; Feng, D; Ginex, T; Kang, D; Lee, KH; Liu, X; Luque, FJ; Murugan, NA; Pannecouque, C; Steitz, TA; Wang, Z; Wei, F; Wu, G; Yang, Y; Zhan, P; Zhang, H; Zhang, J; Zhao, T1
Bartel, K; Bracher, F; Christianson, DW; Herp, D; Jung, M; Marek, M; Müller, M; Ong, N; Porter, NJ; Robaa, D; Romier, C; Schmidtkunz, K; Senger, J; Shaik, TB; Sippl, W; Vögerl, K1
Arnold, E; De Clercq, E; Fang, Z; Feng, D; Kang, D; Liu, X; Pannecouque, C; Pilch, A; Ruiz, FX; Sun, Y; Wang, Z; Wei, F; Zhan, P; Zhao, T1
Guo, HF; Jin, J; Li, ZR; Liu, ZY; Xie, ZS; Xue, ST; Yi, H; Zhang, L1
Fu, L; Huang, H; Li, G; Li, Y; Liu, Y; Lu, H; Lu, Y; Ma, C; Sheng, L; Wang, B; Zhang, B; Zhang, D; Zhao, H1
Ai, W; Chen, Y; Dong, Y; Kang, D; Liang, R; Liu, X; Meng, Q; Pang, J; Sun, Z; Wu, T; Zhan, P; Zhao, T; Zhao, Z1
Chen, SH; Duan, YC; Guan, YY; He, ZH; Jin, LF; Liu, YJ; Ren, HM; Song, Y; Xu, YT; Yuan, H; Zhang, SJ1
Chen, FE; De Clercq, E; Ding, L; Pannecouque, C; Zhuang, C2
Cheng, M; Cui, H; Jiang, H; Li, S; Liu, L; Su, X; Sun, Y; Wu, T; Yin, W; Zhang, Y; Zhao, D; Zhao, L; Zheng, Y1
Chen, Y; Dong, R; Hou, S; Huang, J; Li, H; Liu, C; Liu, X; Lu, T; Tang, W; Wang, X; Xu, J; Zhang, T; Zhang, Y1
Ding, Q; Fan, G; Gao, D; Jiang, Y; Li, Q; Li, W; Ma, C; Mao, L; Xu, G; Yang, S; Zhang, D; Zhang, S; Zhao, J; Zhao, M; Zhu, L1
Bertagnin, C; Du, R; Guizzo, L; Hou, L; Huang, B; Jia, R; Ju, H; Kang, D; Kong, X; Li, P; Liu, X; Loregian, A; Ma, X; Murugan, NA; Poongavanam, V; Zhan, P; Zhang, Y1
Beloglazkina, EK; Ber, AP; Borisova, YA; Chepikova, OE; Erofeev, A; Gorelkin, P; Khazanova, ES; Khudyakov, AD; Kolmogorov, VS; Kovalev, S; Machulkin, AE; Majouga, AG; Nimenko, EA; Pankratov, AA; Petrov, SA; Plotnikova, EA; Pokrovsky, VS; Polshakov, VI; Shafikov, RR; Skvortsov, DA; Smirnova, GB; Uspenskaya, AA; Vaneev, AN; Zamyatnin, AA; Zyk, NU; Zyk, NV1
Ji, J; Liang, R; Liao, H; Liu, X; Pang, J; Shi, X; Tao, Y; Wu, T; Zhan, P; Zhang, J; Zhang, Z; Zhao, F; Zhao, T1
Bong Han, S; Hwang, D; Jung, E; Jung, YS; Kumar Biswas, B; Malpani, YR; Soo Shin, J; Vishakantegowda, AG1
Cheng, M; Qin, Q; Sun, Y; Wang, J; Wang, L; Wu, T; Xue, Y; Yang, H; Yin, W; Zhao, D1
Chen, FE; De Clercq, E; Huang, WJ; Jin, X; Pannecouque, C; Wang, S; Zhang, YX; Zhao, LM1
Bae, S; Cho, Y; Choi, J; Kang, JA; Kim, YC; Lee, D; Lim, C; Park, M; Park, SG; Seo, J1
Chen, Y; Li, Y; Liu, Y; Luan, Y; Wang, K1
Barrow, D; Eissa, AG; Foster, PA; Gee, J; Powell, LE; Simons, C1

Reviews

1 review(s) available for alpha-naphthoflavone and ketoconazole

ArticleYear
Mechanism and inhibition of cytochrome P-450 aromatase.
    Journal of medicinal chemistry, 1990, Volume: 33, Issue:11

    Topics: Affinity Labels; Aromatase; Aromatase Inhibitors; Binding, Competitive; Humans; Molecular Structure; Photochemistry

1990

Other Studies

61 other study(ies) available for alpha-naphthoflavone and ketoconazole

ArticleYear
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
    PLoS medicine, 2006, Volume: 3, Issue:11

    Topics: Animals; Antitubercular Agents; Blood; Cell Line; Humans; In Vitro Techniques; Intracellular Membranes; Macrophages; Mammals; Mice; Microbial Sensitivity Tests; Microsomes, Liver; Mycobacterium; Mycobacterium bovis; Mycolic Acids; Nitroimidazoles; Oxazoles; Treatment Outcome; Tuberculosis

2006
Potential cancer chemopreventive in vitro activities of monomeric xanthone derivatives from the marine algicolous fungus Monodictys putredinis.
    Journal of natural products, 2007, Volume: 70, Issue:3

    Topics: Anticarcinogenic Agents; Aromatase Inhibitors; Ascomycota; Crystallography, X-Ray; Inhibitory Concentration 50; Marine Biology; Molecular Conformation; Molecular Structure; NAD(P)H Dehydrogenase (Quinone); Xanthones

2007
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
    Bioorganic & medicinal chemistry letters, 2010, May-15, Volume: 20, Issue:10

    Topics: Antineoplastic Agents; Aromatase; Aromatase Inhibitors; Binding Sites; Breast Neoplasms; Computer Simulation; Drug Design; Female; Humans; Models, Chemical; Models, Molecular; Structure-Activity Relationship

2010
Synthesis and evaluation of novel potent HCV NS5A inhibitors.
    Bioorganic & medicinal chemistry letters, 2012, Jul-15, Volume: 22, Issue:14

    Topics: Antiviral Agents; Cell Line, Tumor; Cell Survival; Hepacivirus; Humans; Microsomes, Liver; Molecular Structure; Structure-Activity Relationship

2012
Synthesis and evaluation of non-dimeric HCV NS5A inhibitors.
    Bioorganic & medicinal chemistry letters, 2013, Apr-01, Volume: 23, Issue:7

    Topics: Animals; Antiviral Agents; Carbamates; Cell Line; Chlorocebus aethiops; Dose-Response Relationship, Drug; Hepacivirus; Humans; Imidazoles; Microbial Sensitivity Tests; Molecular Structure; Pyrrolidines; Structure-Activity Relationship; Valine; Vero Cells; Viral Nonstructural Proteins; Virus Replication

2013
Potent Hepatitis C Virus NS5A Inhibitors Containing a Benzidine Core.
    ACS medicinal chemistry letters, 2014, Mar-13, Volume: 5, Issue:3

    Topics:

2014
Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.
    Bioorganic & medicinal chemistry letters, 2014, Aug-01, Volume: 24, Issue:15

    Topics: Azetidines; Biological Transport; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Ether-A-Go-Go Potassium Channels; Humans; Molecular Structure; Neurotransmitter Uptake Inhibitors; Phenyl Ethers; Plasma Membrane Neurotransmitter Transport Proteins; Serotonin; Structure-Activity Relationship

2014
Exploration of 3-Aminoazetidines as Triple Reuptake Inhibitors by Bioisosteric Modification of 3-α-Oxyazetidine.
    ACS medicinal chemistry letters, 2014, Sep-11, Volume: 5, Issue:9

    Topics:

2014
Development of (E)-2-((1,4-dimethylpiperazin-2-ylidene)amino)-5-nitro-N-phenylbenzamide, ML336: Novel 2-amidinophenylbenzamides as potent inhibitors of venezuelan equine encephalitis virus.
    Journal of medicinal chemistry, 2014, Oct-23, Volume: 57, Issue:20

    Topics: Animals; Antiviral Agents; Benzamides; Drug Evaluation, Preclinical; Encephalitis Virus, Venezuelan Equine; Encephalomyelitis, Venezuelan Equine; Heterocyclic Compounds, 2-Ring; Mice, Inbred C3H; Mice, Inbred C57BL; Piperazines; Quinazolinones; Small Molecule Libraries; Structure-Activity Relationship; Virus Replication

2014
Phenoxymethyl 1,3-oxazoles and 1,2,4-oxadiazoles as potent and selective agonists of free fatty acid receptor 1 (GPR40).
    Bioorganic & medicinal chemistry letters, 2015, Aug-15, Volume: 25, Issue:16

    Topics: Animals; Binding Sites; Caco-2 Cells; Cytochrome P-450 Enzyme System; Half-Life; Humans; Methylamines; Mice; Molecular Docking Simulation; Oxadiazoles; Oxazoles; Propionates; Protein Binding; Protein Isoforms; Protein Structure, Tertiary; Receptors, G-Protein-Coupled; Structure-Activity Relationship

2015
2-(3-Methoxyphenyl)quinazoline Derivatives: A New Class of Direct Constitutive Androstane Receptor (CAR) Agonists.
    Journal of medicinal chemistry, 2016, 05-26, Volume: 59, Issue:10

    Topics: Constitutive Androstane Receptor; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Enzyme Inhibitors; Hep G2 Cells; Hepatocytes; Humans; Models, Molecular; Molecular Structure; Quinazolines; Receptors, Cytoplasmic and Nuclear; Structure-Activity Relationship

2016
Novel free fatty acid receptor 1 (GPR40) agonists based on 1,3,4-thiadiazole-2-carboxamide scaffold.
    Bioorganic & medicinal chemistry, 2016, 07-01, Volume: 24, Issue:13

    Topics: Amides; Animals; Drug Delivery Systems; Humans; Hypoglycemic Agents; Mice; Microsomes, Liver; Molecular Docking Simulation; Protein Binding; Receptors, G-Protein-Coupled; Thiadiazoles

2016
Discovery of biphenyl imidazole derivatives as potent antifungal agents: Design, synthesis, and structure-activity relationship studies.
    Bioorganic & medicinal chemistry, 2017, 01-15, Volume: 25, Issue:2

    Topics: Antifungal Agents; Biphenyl Compounds; Candida albicans; Cryptococcus neoformans; Dose-Response Relationship, Drug; Drug Discovery; Imidazoles; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Structure-Activity Relationship

2017
Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity.
    Bioorganic & medicinal chemistry letters, 2017, 06-01, Volume: 27, Issue:11

    Topics: Benzoflavones; Binding Sites; Chemical and Drug Induced Liver Injury; Cytochrome P-450 CYP1A2; Cytochrome P-450 CYP1A2 Inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Humans; Ketoconazole; Molecular Docking Simulation; Risk; Tacrine

2017
Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents.
    European journal of medicinal chemistry, 2017, Sep-08, Volume: 137

    Topics: Antifungal Agents; Aspergillus fumigatus; Candida albicans; Cryptococcus neoformans; Dose-Response Relationship, Drug; Drug Design; Heterocyclic Compounds; Hydrocarbons, Aromatic; Microbial Sensitivity Tests; Molecular Structure; Structure-Activity Relationship

2017
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
    Journal of medicinal chemistry, 2018, 01-11, Volume: 61, Issue:1

    Topics: Animals; Drug Design; Enzyme Inhibitors; ERG1 Potassium Channel; HEK293 Cells; Hep G2 Cells; Humans; Inhibitory Concentration 50; Methicillin-Resistant Staphylococcus aureus; Mice; Oxidoreductases; Rats; Safety; Solubility; Structure-Activity Relationship; Water

2018
Constitutive and inducible expression of human cytochrome P450IA1 in yeast Saccharomyces cerevisiae: an alternative enzyme source for in vitro studies.
    Biochemical and biophysical research communications, 1990, Oct-30, Volume: 172, Issue:2

    Topics: Benzoflavones; Cloning, Molecular; Cytochrome P-450 Enzyme System; Escherichia coli; Gene Library; Humans; Ketoconazole; Microsomes; Plasmids; Recombinant Proteins; Saccharomyces cerevisiae; Substrate Specificity

1990
Human hair follicle benzo[a]pyrene and benzo[a]pyrene 7,8-diol metabolism: effect of exposure to a coal tar-containing shampoo.
    The Journal of investigative dermatology, 1987, Volume: 88, Issue:1

    Topics: Aryl Hydrocarbon Hydroxylases; Benzo(a)pyrene; Benzoflavones; Carbon Monoxide; Clotrimazole; Coal Tar; Dihydroxydihydrobenzopyrenes; DNA; Drug Interactions; Enzyme Induction; Hair; Hair Preparations; Humans; Ketoconazole; NADP

1987
Ketoconazole inhibits oxidative modification of low density lipoprotein.
    Atherosclerosis, 1995, Apr-07, Volume: 114, Issue:1

    Topics: Animals; Benzoflavones; Benzopyrene Hydroxylase; Cells, Cultured; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Drug Interactions; Humans; Ketoconazole; Lipoproteins, LDL; Luminescent Measurements; Macrophages, Peritoneal; Methoxsalen; Metyrapone; Mice; Mice, Inbred Strains; Oxidation-Reduction

1995
Steroid metabolism by rabbit olfactory-specific P450 2G1.
    Archives of biochemistry and biophysics, 1994, Volume: 315, Issue:2

    Topics: Androstenedione; Animals; Benzoflavones; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Cytochromes b5; Dihydrotestosterone; Estradiol; Female; Ketoconazole; Kinetics; Male; NADP; Olfactory Mucosa; Progesterone; Rabbits; Steroids; Substrate Specificity; Testosterone

1994
Saccharomyces cerevisiae: an alternative source for human microsomal liver enzymes and its use in drug interaction studies.
    Toxicology, 1993, Oct-05, Volume: 82, Issue:1-3

    Topics: Anticonvulsants; Benzoflavones; Carbamazepine; Cloning, Molecular; Cytochrome P-450 CYP1A2; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; DNA, Complementary; Drug Interactions; Epoxide Hydrolases; Humans; Ketoconazole; Microsomes, Liver; Oxidoreductases, N-Demethylating; Saccharomyces cerevisiae; Valproic Acid

1993
In vitro metabolism of imipramine by brain microsomes: effects of inhibitors and exogenous cytochrome P450 reductase.
    Brain research, 1996, Oct-28, Volume: 738, Issue:1

    Topics: Animals; Benzoflavones; Brain; Imipramine; In Vitro Techniques; Ketoconazole; Male; Microsomes; NADH, NADPH Oxidoreductases; NADPH-Ferrihemoprotein Reductase; Nerve Tissue Proteins; Osmolar Concentration; Quinidine; Rats; Rats, Sprague-Dawley; Time Factors

1996
Halofantrine metabolism in microsomes in man: major role of CYP 3A4 and CYP 3A5.
    The Journal of pharmacy and pharmacology, 1999, Volume: 51, Issue:4

    Topics: Aryl Hydrocarbon Hydroxylases; Benzoflavones; Cytochrome P-450 CYP2C19; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Enzyme Activation; Humans; Isoenzymes; Ketoconazole; Kinetics; Microsomes; Microsomes, Liver; Mixed Function Oxygenases; Phenanthrenes; Saccharomyces cerevisiae; Substrate Specificity

1999
Activation of phenacetin O-deethylase activity by alpha-naphthoflavone in human liver microsomes.
    Xenobiotica; the fate of foreign compounds in biological systems, 1999, Volume: 29, Issue:9

    Topics: Aniline Compounds; Aryl Hydrocarbon Hydroxylases; B-Lymphocytes; Benzoflavones; Cytochrome P-450 CYP1A1; Cytochrome P-450 CYP1A2; Cytochrome P-450 CYP2A6; Cytochrome P-450 CYP2C19; Cytochrome P-450 CYP2C9; Cytochrome P-450 CYP2E1; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Enzyme Activation; Fluvoxamine; Humans; Ketoconazole; Microsomes, Liver; Mixed Function Oxygenases; Recombinant Proteins; Steroid 16-alpha-Hydroxylase; Steroid Hydroxylases

1999
Cytochrome P450-mediated metabolism and cytotoxicity of aflatoxin B(1) in bovine hepatocytes.
    Toxicology in vitro : an international journal published in association with BIBRA, 2000, Volume: 14, Issue:4

    Topics: Aflatoxin B1; Aflatoxin M1; Animals; Benzoflavones; Biotransformation; Cattle; Cell Survival; Cytochrome P-450 CYP1A1; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Enzyme Inhibitors; Female; Ketoconazole; Liver; Steroid Hydroxylases

2000
CYP3A4 is the major CYP isoform mediating the in vitro hydroxylation and demethylation of flunitrazepam.
    Drug metabolism and disposition: the biological fate of chemicals, 2001, Volume: 29, Issue:2

    Topics: Anti-Anxiety Agents; Benzoflavones; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Flunitrazepam; Humans; Hydroxylation; Isoenzymes; Ketoconazole; Kinetics; Methylation; Microsomes, Liver; Mixed Function Oxygenases; Omeprazole; Quinidine; Ritonavir; Sulfaphenazole; Transfection

2001
Metabolism of amiodarone (Part III): identification of rabbit cytochrome P450 isoforms involved in the hydroxylation of mono-N-desethylamiodarone.
    Xenobiotica; the fate of foreign compounds in biological systems, 2001, Volume: 31, Issue:5

    Topics: Amiodarone; Animals; Anti-Anxiety Agents; Anti-Arrhythmia Agents; Aryl Hydrocarbon Hydroxylases; Benzoflavones; Chromatography, High Pressure Liquid; Cimetidine; Cyclosporine; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Enzyme Inhibitors; Ketoconazole; Kinetics; Microsomes, Liver; Midazolam; Models, Chemical; Oxidoreductases, N-Demethylating; Protein Isoforms; Quinidine; Rabbits; Rifampin; Time Factors

2001
Specific interactions of steroids, arylhydrocarbons and flavonoids with progesterone receptors from the cytosol of the fungus Rhizopus nigricans.
    The Journal of steroid biochemistry and molecular biology, 2004, Volume: 91, Issue:4-5

    Topics: Allosteric Regulation; Antifungal Agents; Benzoflavones; Binding Sites; Binding, Competitive; Cytosol; Drug Interactions; Flavonoids; Hydroxylation; Ketoconazole; Kinetics; Ligands; Receptors, Progesterone; Rhizopus; Steroids; Substrate Specificity

2004
Intestinal metabolism of PAH: in vitro demonstration and study of its impact on PAH transfer through the intestinal epithelium.
    Environmental research, 2005, Volume: 98, Issue:1

    Topics: Benzo(a)pyrene; Benzoflavones; Caco-2 Cells; Cell Differentiation; Cell Membrane Permeability; Cell Survival; Chromatography, Thin Layer; Colon; Cytochrome P-450 Enzyme Inhibitors; Enzyme Inhibitors; Histocytochemistry; Humans; Intestinal Absorption; Intestinal Mucosa; Isoenzymes; Ketoconazole; Kinetics; Phenanthrenes; Pyrenes

2005
Metabolism and metabolic inhibition of gambogic acid in rat liver microsomes.
    Acta pharmacologica Sinica, 2006, Volume: 27, Issue:9

    Topics: Animals; Benzoflavones; Cytochrome P-450 CYP1A2 Inhibitors; Cytochrome P-450 CYP3A Inhibitors; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Ketoconazole; Microsomes, Liver; Rats; Rats, Sprague-Dawley; Sulfaphenazole; Xanthones

2006
CYP3A4 mediated in vitro metabolism of vinflunine in human liver microsomes.
    Acta pharmacologica Sinica, 2007, Volume: 28, Issue:1

    Topics: Aryl Hydrocarbon Hydroxylases; Benzoflavones; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Ditiocarb; Humans; Ketoconazole; Microsomes, Liver; Molecular Structure; Quinidine; Sulfaphenazole; Tranylcypromine; Vinblastine

2007
Cytotoxicity of ginkgolic acid in HepG2 cells and primary rat hepatocytes.
    Toxicology letters, 2009, Jun-22, Volume: 187, Issue:3

    Topics: Animals; Benzoflavones; beta-Naphthoflavone; Cell Line, Tumor; Cell Survival; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Fomepizole; Hepatocytes; Humans; Isoenzymes; Ketoconazole; Liver; Male; Microsomes, Liver; Pyrazoles; Quinine; Rats; Rats, Sprague-Dawley; Salicylates; Sulfaphenazole

2009
[Enzyme kinetics of ligustilide metabolism in rat liver microsomes].
    Yao xue xue bao = Acta pharmaceutica Sinica, 2009, Volume: 44, Issue:4

    Topics: 4-Butyrolactone; Animals; Benzoflavones; Cytochrome P-450 CYP1A2; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Cytochromes; Ketoconazole; Kinetics; Male; Microsomes, Liver; Rats; Rats, Sprague-Dawley; Trimethoprim

2009
Hepatic cytochrome P450s attenuate the cytotoxicity induced by leflunomide and its active metabolite A77 1726 in primary cultured rat hepatocytes.
    Toxicological sciences : an official journal of the Society of Toxicology, 2011, Volume: 122, Issue:2

    Topics: Aniline Compounds; Animals; Benzoflavones; Biomarkers; Cell Survival; Cells, Cultured; Crotonates; Cytochrome P-450 Enzyme System; Hepatocytes; Hydroxybutyrates; Inactivation, Metabolic; Isoxazoles; Ketoconazole; Leflunomide; Liver; Male; Nitriles; Primary Cell Culture; Proadifen; Rats; Rats, Sprague-Dawley; Ticlopidine; Toluidines; Triazoles

2011
Effects of cytochrome P450 inhibitors on peroxidase activity.
    Neuro endocrinology letters, 2012, Volume: 33 Suppl 3

    Topics: Benzoflavones; Cytochrome P-450 Enzyme Inhibitors; Disulfiram; Ditiocarb; Ellipticines; Enzyme Activation; Enzyme Inhibitors; Horseradish Peroxidase; Humans; Ketoconazole; Metyrapone; Piperonyl Butoxide; Proadifen; Quinidine; Structure-Activity Relationship; Substrate Specificity; Sulfaphenazole; Triazoles; Troleandomycin

2012
Inhibition of cytochrome P450s enhances (+)-usnic acid cytotoxicity in primary cultured rat hepatocytes.
    Journal of applied toxicology : JAT, 2014, Volume: 34, Issue:8

    Topics: Animals; Benzoflavones; Benzofurans; Cells, Cultured; Chemical and Drug Induced Liver Injury; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dietary Supplements; Enzyme Inhibitors; Hepatocytes; Ketoconazole; Liver; Male; Mitochondria; Proadifen; Rats; Rats, Sprague-Dawley; Ticlopidine

2014
The role of CYP 3A4 and 1A1 in amiodarone-induced hepatocellular toxicity.
    Toxicology letters, 2016, Jun-24, Volume: 253

    Topics: Activation, Metabolic; Amiodarone; Anti-Arrhythmia Agents; Benzoflavones; Cell Survival; Chemical and Drug Induced Liver Injury; Cytochrome P-450 CYP1A1; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Dose-Response Relationship, Drug; Hep G2 Cells; Hepatocytes; Humans; Ketoconazole; Time Factors; Transfection

2016
Novel Tetrahydropyrido[4,3-d]pyrimidines as Potent Inhibitors of Chaperone Heat Shock Protein 90.
    Journal of medicinal chemistry, 2016, 12-08, Volume: 59, Issue:23

    Topics: Animals; Antineoplastic Agents; Cell Proliferation; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; HCT116 Cells; HSP90 Heat-Shock Proteins; Humans; Male; Mice; Mice, Nude; Models, Molecular; Molecular Structure; Neoplasms, Experimental; Pyridines; Pyrimidines; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Xenograft Model Antitumor Assays

2016
Design, synthesis and evaluation of benzoheterocycle analogues as potent antifungal agents targeting CYP51.
    Bioorganic & medicinal chemistry, 2018, 07-23, Volume: 26, Issue:12

    Topics: Antifungal Agents; Aspergillus fumigatus; Binding Sites; Candida albicans; Catalytic Domain; Cryptococcus neoformans; Drug Design; Drug Resistance, Fungal; Drug Stability; Fluconazole; Fungal Proteins; Gas Chromatography-Mass Spectrometry; Humans; Microbial Sensitivity Tests; Molecular Docking Simulation; Protein Isoforms; Sterol 14-Demethylase; Sterols; Structure-Activity Relationship; Triazoles

2018
Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo.
    European journal of medicinal chemistry, 2018, Sep-05, Volume: 157

    Topics: Animals; Antineoplastic Agents; Cell Line; Cell Proliferation; Cell Survival; Colonic Neoplasms; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Guanidine; Hedgehog Proteins; Humans; Mice; Mice, Nude; Molecular Structure; Neoplasms, Experimental; NIH 3T3 Cells; Structure-Activity Relationship; Thiourea

2018
Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
    Journal of medicinal chemistry, 2019, 02-14, Volume: 62, Issue:3

    Topics: Animals; Anti-HIV Agents; Binding Sites; Cell Line, Tumor; Furans; HIV Reverse Transcriptase; HIV-1; Humans; Male; Microbial Sensitivity Tests; Molecular Dynamics Simulation; Molecular Structure; Pyrimidines; Rats, Wistar; Reverse Transcriptase Inhibitors; Structure-Activity Relationship

2019
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
    Journal of medicinal chemistry, 2019, 02-14, Volume: 62, Issue:3

    Topics: Acetylation; Animals; Catalytic Domain; Cells, Cultured; Crystallography, X-Ray; Histone Deacetylase 6; Histone Deacetylase Inhibitors; HL-60 Cells; Humans; Hydroxamic Acids; In Vitro Techniques; Microsomes, Liver; Molecular Docking Simulation; Molecular Structure; Phenothiazines; Structure-Activity Relationship; Zebrafish

2019
Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
    Journal of medicinal chemistry, 2020, 02-13, Volume: 63, Issue:3

    Topics: Animals; Anti-HIV Agents; Cell Line; Crystallography, X-Ray; Drug Discovery; ERG1 Potassium Channel; Female; Fluorine; HIV Reverse Transcriptase; HIV-1; Humans; Male; Mice; Microsomes, Liver; Molecular Structure; Protein Binding; Pyrimidines; Rats, Wistar; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Thiophenes

2020
Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties.
    European journal of medicinal chemistry, 2020, Aug-15, Volume: 200

    Topics: Animals; Benzofurans; Bone Morphogenetic Protein 2; Caco-2 Cells; Disease Models, Animal; Dose-Response Relationship, Drug; Humans; Mice; Mice, Inbred BALB C; Molecular Structure; Osteoporosis; Ovariectomy; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Thiophenes; Zebrafish

2020
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
    Journal of medicinal chemistry, 2020, 09-10, Volume: 63, Issue:17

    Topics: Animals; Chlorocebus aethiops; Drug Design; Female; Hep G2 Cells; Humans; Mice; Microbial Sensitivity Tests; Molecular Conformation; Mycobacterium tuberculosis; Oxazolidinones; Safety; Tuberculosis, Multidrug-Resistant; Vero Cells

2020
Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
    Journal of medicinal chemistry, 2020, 10-08, Volume: 63, Issue:19

    Topics: Animals; Carbon-13 Magnetic Resonance Spectroscopy; Gout; HEK293 Cells; Humans; Hyperuricemia; Mass Spectrometry; Mice; Organic Anion Transporters; Organic Cation Transport Proteins; Proton Magnetic Resonance Spectroscopy; Rats; Structure-Activity Relationship; Uricosuric Agents

2020
Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
    European journal of medicinal chemistry, 2021, Aug-05, Volume: 220

    Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Proliferation; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Histone Deacetylases; Histone Demethylases; Humans; Microsomes, Liver; Molecular Docking Simulation; Molecular Structure; Rats; Stomach Neoplasms; Structure-Activity Relationship; Tumor Cells, Cultured

2021
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
    Journal of medicinal chemistry, 2021, 07-22, Volume: 64, Issue:14

    Topics: Animals; Anti-HIV Agents; Dose-Response Relationship, Drug; Female; HIV Reverse Transcriptase; HIV-1; Humans; Male; Mice; Microbial Sensitivity Tests; Microsomes, Liver; Models, Molecular; Molecular Structure; Pyrimidines; Rats; Rats, Sprague-Dawley; Reverse Transcriptase Inhibitors; Structure-Activity Relationship

2021
Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
    European journal of medicinal chemistry, 2021, Dec-05, Volume: 225

    Topics: Antifungal Agents; Candida albicans; Dose-Response Relationship, Drug; Drug Design; Drug Resistance, Fungal; Fluconazole; Fungicides, Industrial; Humans; Microbial Sensitivity Tests; Molecular Structure; Structure-Activity Relationship; Thiophenes

2021
Discovery of
    Journal of medicinal chemistry, 2021, 09-09, Volume: 64, Issue:17

    Topics: Administration, Oral; Animals; Antineoplastic Agents; Area Under Curve; Catalytic Domain; Cell Line, Tumor; Cyclin-Dependent Kinase 9; Half-Life; Humans; Mice; Molecular Structure; Protein Binding; Protein Kinase Inhibitors; Structure-Activity Relationship; Xenograft Model Antitumor Assays

2021
Discovery of 1-Amino-1
    Journal of medicinal chemistry, 2021, 11-11, Volume: 64, Issue:21

    Topics: Agammaglobulinaemia Tyrosine Kinase; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cytochrome P-450 Enzyme Inhibitors; Drug Discovery; Humans; Imidazoles; Molecular Docking Simulation; Protein Kinase Inhibitors; Signal Transduction; Structure-Activity Relationship

2021
Identification of C5-NH
    Journal of medicinal chemistry, 2021, 12-23, Volume: 64, Issue:24

    Topics: Animals; Antiviral Agents; Biological Availability; Chick Embryo; Computer Simulation; Half-Life; Influenza A Virus, H5N1 Subtype; Mice; Molecular Docking Simulation; Molecular Dynamics Simulation; Neuraminidase; Oseltamivir; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship

2021
Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate.
    Journal of medicinal chemistry, 2021, 12-09, Volume: 64, Issue:23

    Topics: Antigens, Surface; Cell Line, Tumor; Coordination Complexes; Glutamate Carboxypeptidase II; Humans; Male; Microsomes, Liver; Oligopeptides; Prostatic Neoplasms; Reactive Oxygen Species; Xenograft Model Antitumor Assays

2021
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
    Journal of medicinal chemistry, 2022, 02-10, Volume: 65, Issue:3

    Topics: Animals; Anti-HIV Agents; Binding Sites; Cell Survival; Cytochrome P-450 Enzyme System; Drug Design; Drug Resistance, Viral; Drug Stability; Female; Half-Life; HIV Reverse Transcriptase; HIV-1; Humans; Mice; Molecular Docking Simulation; Mutation; Pyridines; Pyrimidines; Solubility; Structure-Activity Relationship

2022
Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
    Journal of medicinal chemistry, 2022, 03-10, Volume: 65, Issue:5

    Topics: Animals; Gout; Humans; Hyperuricemia; Mice; Organic Anion Transporters; Organic Cation Transport Proteins; Uric Acid

2022
Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
    Bioorganic & medicinal chemistry letters, 2022, 05-15, Volume: 64

    Topics: Animals; Antiviral Agents; Capsid; Enterovirus; Enterovirus Infections; Purines; Rats; Rhinovirus; Virus Replication

2022
Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
    European journal of medicinal chemistry, 2022, Aug-05, Volume: 238

    Topics: Animals; Antineoplastic Agents; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Drug Design; Drug Screening Assays, Antitumor; Female; Humans; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Pyrimidines; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Tripartite Motif Proteins; Ubiquitin-Protein Ligases

2022
Structure-Based Discovery of Novel NH
    Journal of medicinal chemistry, 2022, 06-23, Volume: 65, Issue:12

    Topics: Anti-HIV Agents; Biphenyl Compounds; Drug Design; Heterocyclic Compounds, 1-Ring; HIV Reverse Transcriptase; HIV-1; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship

2022
Entry inhibition of hepatitis B virus using cyclosporin O derivatives with peptoid side chain incorporation.
    Bioorganic & medicinal chemistry, 2022, 08-15, Volume: 68

    Topics: Antiviral Agents; Cyclosporins; Hepatitis B; Hepatitis B virus; Humans; Imidazoles; Liver Neoplasms; Organic Anion Transporters, Sodium-Dependent; Peptoids; Sulfonamides; Symporters; Thiophenes; Virus Internalization

2022
Design, synthesis and antitumor activity study of a gemcitabine prodrug conjugated with a HDAC6 inhibitor.
    Bioorganic & medicinal chemistry letters, 2022, 09-15, Volume: 72

    Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Deoxycytidine; Gemcitabine; Histone Deacetylase 6; Humans; Mice; Prodrugs; Xenograft Model Antitumor Assays

2022
4th generation nonsteroidal aromatase inhibitors: An iterative SAR-guided design, synthesis, and biological evaluation towards picomolar dual binding inhibitors.
    European journal of medicinal chemistry, 2022, Oct-05, Volume: 240

    Topics: Aromatase; Aromatase Inhibitors; Breast Neoplasms; Female; Humans; Receptors, Estrogen; Triazoles

2022