Page last updated: 2024-08-07 15:55:19
Aromatase
An aromatase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P11511]
Synonyms
EC 1.14.14.14;
CYPXIX;
Cytochrome P-450AROM;
Cytochrome P450 19A1;
Estrogen synthase
Research
Bioassay Publications (164)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 10 (6.10) | 18.7374 |
| 1990's | 21 (12.80) | 18.2507 |
| 2000's | 51 (31.10) | 29.6817 |
| 2010's | 72 (43.90) | 24.3611 |
| 2020's | 10 (6.10) | 2.80 |
Compounds (119)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| melatonin | Homo sapiens (human) | IC50 | 11.3000 | 1 | 1 |
| naringenin | Homo sapiens (human) | Ki | 0.0000 | 1 | 1 |
| 7-hydroxyflavanone | Homo sapiens (human) | IC50 | 3.8000 | 2 | 2 |
| 7-nitroindazole | Homo sapiens (human) | IC50 | 0.7000 | 1 | 3 |
| tyrphostin a23 | Homo sapiens (human) | IC50 | 70.6000 | 1 | 1 |
| aminoglutethimide | Homo sapiens (human) | IC50 | 70,459,513.2611 | 39 | 40 |
| aminoglutethimide | Homo sapiens (human) | Ki | 1.3615 | 13 | 13 |
| anastrozole | Homo sapiens (human) | IC50 | 0.1443 | 13 | 13 |
| anastrozole | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
| clotrimazole | Homo sapiens (human) | IC50 | 0.0018 | 1 | 1 |
| fluconazole | Homo sapiens (human) | IC50 | 22.0000 | 1 | 1 |
| fluorouracil | Homo sapiens (human) | IC50 | 0.6300 | 1 | 1 |
| ketoconazole | Homo sapiens (human) | IC50 | 17.5615 | 12 | 13 |
| ketoconazole | Homo sapiens (human) | Ki | 21.9327 | 2 | 3 |
| letrozole | Homo sapiens (human) | IC50 | 1.4476 | 40 | 41 |
| letrozole | Homo sapiens (human) | Ki | 0.0011 | 2 | 2 |
| metyrapone | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| miconazole | Homo sapiens (human) | IC50 | 0.6000 | 1 | 1 |
| nimesulide | Homo sapiens (human) | IC50 | 27.0000 | 1 | 1 |
| masoprocol | Homo sapiens (human) | IC50 | 0.0110 | 1 | 1 |
| n-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide | Homo sapiens (human) | IC50 | 0.6800 | 2 | 2 |
| sb 206553 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| estrone | Homo sapiens (human) | Ki | 2.5000 | 1 | 1 |
| androstenedione | Homo sapiens (human) | IC50 | 0.2800 | 2 | 2 |
| androstenedione | Homo sapiens (human) | Ki | 0.0275 | 2 | 2 |
| flavanone | Homo sapiens (human) | IC50 | 18.1250 | 4 | 4 |
| dihydrotestosterone | Homo sapiens (human) | Ki | 0.8850 | 2 | 2 |
| flavone | Homo sapiens (human) | IC50 | 6.0027 | 3 | 3 |
| herniarin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| formestane | Homo sapiens (human) | IC50 | 4.7828 | 13 | 13 |
| formestane | Homo sapiens (human) | Ki | 0.1432 | 5 | 5 |
| alpha-naphthoflavone | Homo sapiens (human) | IC50 | 1.0350 | 2 | 2 |
| alpha-naphthoflavone | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| 4,6-androstadiene-3,17-dione | Homo sapiens (human) | Ki | 0.0170 | 1 | 1 |
| boldenone | Homo sapiens (human) | Ki | 0.2600 | 1 | 1 |
| 1,4-androstadiene-3,17-dione | Homo sapiens (human) | IC50 | 0.4150 | 1 | 2 |
| 1,4-androstadiene-3,17-dione | Homo sapiens (human) | Ki | 0.3258 | 6 | 6 |
| testolactone | Homo sapiens (human) | Ki | 35.0000 | 1 | 1 |
| dazoxiben | Homo sapiens (human) | IC50 | 1.1000 | 1 | 1 |
| n-(4-nitrophenacyl)imidazole | Homo sapiens (human) | IC50 | 0.1900 | 1 | 1 |
| rogletimide | Homo sapiens (human) | IC50 | 20.0000 | 3 | 3 |
| rogletimide | Homo sapiens (human) | Ki | 5.4000 | 3 | 3 |
| fadrozole | Homo sapiens (human) | IC50 | 0.0324 | 31 | 36 |
| fadrozole | Homo sapiens (human) | Ki | 0.0009 | 4 | 4 |
| aromasil | Homo sapiens (human) | IC50 | 0.1701 | 8 | 8 |
| aromasil | Homo sapiens (human) | Ki | 0.0181 | 2 | 2 |
| liarozole | Homo sapiens (human) | IC50 | 0.0248 | 2 | 2 |
| azalanstat | Homo sapiens (human) | Ki | 0.0076 | 1 | 1 |
| 1,1-bis(4-hydroxyphenyl)-2-phenylbut-1-ene | Homo sapiens (human) | IC50 | 24.8867 | 3 | 3 |
| 4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol | Homo sapiens (human) | IC50 | 530.0000 | 1 | 1 |
| ursolic acid | Homo sapiens (human) | IC50 | 32.0000 | 1 | 1 |
| 2-methylestradiol | Homo sapiens (human) | Ki | 0.1000 | 1 | 1 |
| 2-fluoroestradiol | Homo sapiens (human) | Ki | 0.1000 | 1 | 1 |
| 4-methylquinolin-2(1H)-one | Homo sapiens (human) | IC50 | 250.4667 | 2 | 3 |
| dehydroleucodine | Homo sapiens (human) | IC50 | 0.0150 | 1 | 1 |
| 1-benzylimidazole | Homo sapiens (human) | IC50 | 0.1500 | 1 | 1 |
| 7-(diethylamino)-1-benzopyran-2-one | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| monocerin | Homo sapiens (human) | IC50 | 16.2000 | 1 | 1 |
| androst-2-en-17-one | Homo sapiens (human) | IC50 | 1.7330 | 1 | 1 |
| androst-2-en-17-one | Homo sapiens (human) | Ki | 9.5010 | 1 | 1 |
| androsta-1,4,6-triene-3,17-dione | Homo sapiens (human) | Ki | 0.0912 | 2 | 2 |
| liquiritigenin | Homo sapiens (human) | IC50 | 1.2200 | 2 | 2 |
| 7-(4'-amino)phenylthioandrostenedione | Homo sapiens (human) | Ki | 0.0180 | 2 | 2 |
| cyclohexylaminoglutethimide | Homo sapiens (human) | IC50 | 1.6833 | 1 | 3 |
| cgp 47645 | Homo sapiens (human) | IC50 | 0.0617 | 1 | 1 |
| 19-hydroxy-4-androsten-17-one | Homo sapiens (human) | IC50 | 0.1227 | 3 | 3 |
| 19-hydroxy-4-androsten-17-one | Homo sapiens (human) | Ki | 0.0104 | 3 | 3 |
| 7-((4'-aminophenyl)thio)-1,4-androstadiene-3,17-dione | Homo sapiens (human) | Ki | 0.0099 | 1 | 1 |
| abiraterone | Homo sapiens (human) | IC50 | 25.0000 | 3 | 3 |
| isoflavanone | Homo sapiens (human) | IC50 | 29.0000 | 1 | 1 |
| ym 511 | Homo sapiens (human) | IC50 | 0.0005 | 5 | 5 |
| dihydroresveratrol | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| sorafenib | Homo sapiens (human) | IC50 | 0.1269 | 1 | 7 |
| naringenin | Homo sapiens (human) | IC50 | 2.9493 | 10 | 10 |
| naringin | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| sb 221284 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| arachidonic acid | Homo sapiens (human) | IC50 | 28.2000 | 1 | 1 |
| resveratrol | Homo sapiens (human) | IC50 | 30.2267 | 6 | 6 |
| resveratrol | Homo sapiens (human) | Ki | 41.6700 | 1 | 1 |
| docosahexaenoate | Homo sapiens (human) | IC50 | 33.2000 | 1 | 1 |
| oleic acid | Homo sapiens (human) | IC50 | 32.7000 | 1 | 1 |
| eicosapentaenoic acid | Homo sapiens (human) | IC50 | 53.2000 | 1 | 1 |
| afimoxifene | Homo sapiens (human) | IC50 | 530.0000 | 1 | 1 |
| ketoconazole | Homo sapiens (human) | IC50 | 1.3026 | 5 | 6 |
| benzyloxycarbonylleucyl-leucyl-leucine aldehyde | Homo sapiens (human) | IC50 | 0.0440 | 1 | 1 |
| 7-methoxyflavone | Homo sapiens (human) | IC50 | 0.5100 | 1 | 1 |
| posaconazole | Homo sapiens (human) | IC50 | 8.4000 | 1 | 1 |
| isoliquiritigenin | Homo sapiens (human) | IC50 | 3.8000 | 1 | 1 |
| 4-(3-pyridinyloxy)benzene-1,2-dicarbonitrile | Homo sapiens (human) | IC50 | 5.0300 | 1 | 1 |
| 4-(1H-imidazol-1-ylmethyl)benzonitrile | Homo sapiens (human) | IC50 | 0.5796 | 4 | 4 |
| 4-aminostilbene | Homo sapiens (human) | IC50 | 22.0000 | 1 | 1 |
| cis-resveratrol | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| 2,4-Di(3-pyridyl)-1,3-thiazole | Homo sapiens (human) | IC50 | 0.0040 | 1 | 1 |
| sb 242084 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 7-methoxy-2-(4-methoxyphenyl)-3,4-dihydro-2H-1-benzopyran-4-one | Homo sapiens (human) | IC50 | 1.8600 | 1 | 1 |
| calceolarioside b | Homo sapiens (human) | IC50 | 35.3000 | 1 | 1 |
| quercetin | Homo sapiens (human) | IC50 | 6.0060 | 2 | 2 |
| biochanin a | Homo sapiens (human) | IC50 | 5,647,400,049.0017 | 6 | 6 |
| biochanin a | Homo sapiens (human) | Ki | 12.0000 | 4 | 4 |
| apigenin | Homo sapiens (human) | IC50 | 3.2750 | 4 | 4 |
| linoleic acid | Homo sapiens (human) | IC50 | 48.0000 | 1 | 1 |
| gossypetin | Homo sapiens (human) | IC50 | 11.0000 | 1 | 1 |
| alpha-linolenic acid | Homo sapiens (human) | IC50 | 44.2000 | 1 | 1 |
| genistein | Homo sapiens (human) | Ki | 111.5000 | 2 | 2 |
| chrysin | Homo sapiens (human) | IC50 | 0.6670 | 3 | 3 |
| chrysin | Homo sapiens (human) | Ki | 2.6000 | 1 | 1 |
| galangin | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| mangostin | Homo sapiens (human) | IC50 | 20.7000 | 1 | 1 |
| myricetin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| daidzein | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| 7-hydroxyflavone | Homo sapiens (human) | IC50 | 6.3768 | 3 | 3 |
| 4',7-dihydroxyflavone | Homo sapiens (human) | IC50 | 0.0020 | 1 | 1 |
| irosustat | Homo sapiens (human) | IC50 | 0.3000 | 3 | 3 |
| broussonin a | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| Isolicoflavonol | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | IC50 | 0.0180 | 1 | 1 |
| 6,7-dihydroxyflavone | Homo sapiens (human) | IC50 | 0.0087 | 1 | 1 |
| Isoliquiritigenin 4,4'-dimethyl ether | Homo sapiens (human) | IC50 | 351.7000 | 1 | 1 |
| gamma-mangostin | Homo sapiens (human) | IC50 | 5.9350 | 2 | 2 |
| vx680 | Homo sapiens (human) | Ki | 0.0805 | 1 | 6 |
| docosapentaenoic acid | Homo sapiens (human) | IC50 | 16.8000 | 1 | 1 |
| gdp 366 | Homo sapiens (human) | IC50 | 0.1830 | 1 | 4 |
| vorozole | Homo sapiens (human) | IC50 | 0.0190 | 4 | 4 |
| bis(7)-tacrine | Homo sapiens (human) | IC50 | 2.9000 | 1 | 3 |
| morachalcone a | Homo sapiens (human) | IC50 | 4.6000 | 1 | 1 |
| 3-oxo-12-ursen-28-oic acid | Homo sapiens (human) | IC50 | 500.0000 | 1 | 1 |
| plomestane | Homo sapiens (human) | IC50 | 0.0562 | 1 | 1 |
| plomestane | Homo sapiens (human) | Ki | 0.0085 | 3 | 3 |
| abyssinone ii | Homo sapiens (human) | IC50 | 34.5167 | 3 | 3 |
| 4-hydroxy-n-desmethyltamoxifen | Homo sapiens (human) | IC50 | 7.0250 | 4 | 4 |
| garcinone e | Homo sapiens (human) | IC50 | 25.1000 | 1 | 1 |
| abt 869 | Homo sapiens (human) | IC50 | 0.0418 | 1 | 6 |
| ludartin | Homo sapiens (human) | IC50 | 0.0550 | 1 | 1 |
| Moracin P | Homo sapiens (human) | IC50 | 10.6000 | 1 | 1 |
| osilodrostat | Homo sapiens (human) | IC50 | 2.1109 | 4 | 4 |
| mulberrofuran g | Homo sapiens (human) | IC50 | 7.5000 | 1 | 1 |
Drugs with Other Measurements
New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
Design, synthesis and evaluation of 4-imidazolylflavans as new leads for aromatase inhibition.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
An overview on Estrogen receptors signaling and its ligands in breast cancer.European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
Evaluation of synthesized coumarin derivatives on aromatase inhibitory activity.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 27, Issue:12, 2017
Recent Progress in the Discovery of Next Generation Inhibitors of Aromatase from the Structure-Function Perspective.Journal of medicinal chemistry, , 06-09, Volume: 59, Issue:11, 2016
Developing steroidal aromatase inhibitors-an effective armament to win the battle against breast cancer.European journal of medicinal chemistry, , Nov-13, Volume: 105, 2015
Lead optimization of 4-imidazolylflavans: new promising aromatase inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
An efficient steroid pharmacophore-based strategy to identify new aromatase inhibitors.European journal of medicinal chemistry, , Volume: 44, Issue:10, 2009
Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities.Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009
Synthesis of 6- or 4-functionalized indoles via a reductive cyclization approach and evaluation as aromatase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 2008
Synthesis and biological evaluation of (+/-)-abyssinone II and its analogues as aromatase inhibitors for chemoprevention of breast cancer.Journal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
Synthesis and biological evaluation of 5-[(aryl)(1H-imidazol-1-yl)methyl]-1H-indoles: potent and selective aromatase inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
Benzofuran- and furan-2-yl-(phenyl)-3-pyridylmethanols: synthesis and inhibition of P450 aromatase.Journal of enzyme inhibition and medicinal chemistry, , Volume: 20, Issue:2, 2005
Lead optimization of 7-benzyloxy 2-(4'-pyridylmethyl)thio isoflavone aromatase inhibitors.Bioorganic & medicinal chemistry, , Dec-01, Volume: 13, Issue:23, 2005
Synthesis and characterization of azole isoflavone inhibitors of aromatase.Bioorganic & medicinal chemistry, , Jun-02, Volume: 13, Issue:12, 2005
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.Journal of medicinal chemistry, , Jul-29, Volume: 47, Issue:16, 2004
Preparation and pharmacological profile of 7-(alpha-azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors.Bioorganic & medicinal chemistry letters, , May-05, Volume: 13, Issue:9, 2003
New aromatase inhibitors. Synthesis and inhibitory activity of pyridinyl-substituted flavanone derivatives.Bioorganic & medicinal chemistry letters, , Apr-08, Volume: 12, Issue:7, 2002
Design, synthesis and evaluation of 4-imidazolylflavans as new leads for aromatase inhibition.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase.Journal of medicinal chemistry, , Mar-01, Volume: 44, Issue:5, 2001
Aromatase inhibitors from Broussonetia papyrifera.Journal of natural products, , Volume: 64, Issue:10, 2001
1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.Journal of medicinal chemistry, , May-04, Volume: 43, Issue:9, 2000
1-[(Benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles - potent competitive inhibitors of aromatase.Bioorganic & medicinal chemistry letters, , Jul-19, Volume: 9, Issue:14, 1999
Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
Aromatase inhibitors: synthesis, biological activity, and binding mode of azole-type compounds.Journal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Synthesis and aromatase inhibition of 3-cycloalkyl-substituted 3-(4-aminophenyl)piperidine-2,6-diones.Journal of medicinal chemistry, , Jun-12, Volume: 35, Issue:12, 1992
New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.Journal of medicinal chemistry, , Volume: 34, Issue:9, 1991
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.Journal of medicinal chemistry, , Volume: 34, Issue:2, 1991
Crystallographic and molecular modeling studies on 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione and its butyl analogue, inhibitors of mammalian aromatase. Comparison with natural substrates: prediction of enantioselectivity for N-alkyl derivatives.Journal of medicinal chemistry, , Volume: 33, Issue:9, 1990
Mechanism and inhibition of cytochrome P-450 aromatase.Journal of medicinal chemistry, , Volume: 33, Issue:11, 1990
Analogues of aminoglutethimide based on 1-phenyl-3-azabicyclo[3.1.0]hexane-2,4-dione: selective inhibition of aromatase activity.Journal of medicinal chemistry, , Volume: 31, Issue:5, 1988
Analogues of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents.Journal of medicinal chemistry, , Volume: 30, Issue:9, 1987
Aromatase inhibitors. Synthesis and evaluation of mammary tumor inhibiting activity of 3-alkylated 3-(4-aminophenyl)piperidine-2,6-diones.Journal of medicinal chemistry, , Volume: 29, Issue:8, 1986
Synthesis and biochemical evaluation of analogues of aminoglutethimide based on phenylpyrrolidine-2,5-dione.Journal of medicinal chemistry, , Volume: 29, Issue:4, 1986
Analogues of aminoglutethimide: selective inhibition of aromatase.Journal of medicinal chemistry, , Volume: 28, Issue:2, 1985
An overview on Estrogen receptors signaling and its ligands in breast cancer.European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
Studies on non-steroidal inhibitors of aromatase enzyme; 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl)thiazole derivatives.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Recent Progress in the Discovery of Next Generation Inhibitors of Aromatase from the Structure-Function Perspective.Journal of medicinal chemistry, , 06-09, Volume: 59, Issue:11, 2016
Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health.Journal of medicinal chemistry, , Oct-08, Volume: 58, Issue:19, 2015
Development of a new class of aromatase inhibitors: design, synthesis and inhibitory activity of 3-phenylchroman-4-one (isoflavanone) derivatives.Bioorganic & medicinal chemistry, , Apr-15, Volume: 20, Issue:8, 2012
Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrol.Bioorganic & medicinal chemistry, , Apr-01, Volume: 20, Issue:7, 2012
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
Synthesis of 6- or 4-functionalized indoles via a reductive cyclization approach and evaluation as aromatase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 2008
Potent CYP19 (aromatase) 1-[(benzofuran-2-yl)(phenylmethyl)pyridine, -imidazole, and -triazole inhibitors: synthesis and biological evaluation.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
Benzofuran- and furan-2-yl-(phenyl)-3-pyridylmethanols: synthesis and inhibition of P450 aromatase.Journal of enzyme inhibition and medicinal chemistry, , Volume: 20, Issue:2, 2005
Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 26, Issue:23, 2016
Synthesis and molecular docking of 1,2,3-triazole-based sulfonamides as aromatase inhibitors.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Development of a new class of aromatase inhibitors: design, synthesis and inhibitory activity of 3-phenylchroman-4-one (isoflavanone) derivatives.Bioorganic & medicinal chemistry, , Apr-15, Volume: 20, Issue:8, 2012
Discovery of a novel class of aldol-derived 1,2,3-triazoles: potent and selective inhibitors of human cytochrome P450 19A1 (aromatase).Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Radical scavenging and antioxidant activities of isocoumarins and a phthalide from the endophytic fungus Colletotrichum sp.Journal of natural products, , Jan-28, Volume: 74, Issue:1, 2011
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
Screening of herbal constituents for aromatase inhibitory activity.Bioorganic & medicinal chemistry, , Sep-15, Volume: 16, Issue:18, 2008
Monodictyochromes A and B, dimeric xanthone derivatives from the marine algicolous fungus Monodictys putredinis.Journal of natural products, , Volume: 71, Issue:11, 2008
Potential cancer chemopreventive in vitro activities of monomeric xanthone derivatives from the marine algicolous fungus Monodictys putredinis.Journal of natural products, , Volume: 70, Issue:3, 2007
Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
3- and 4-pyridylalkyl adamantanecarboxylates: inhibitors of human cytochrome P450(17 alpha) (17 alpha-hydroxylase/C17,20-lyase). Potential nonsteroidal agents for the treatment of prostatic cancer.Journal of medicinal chemistry, , Aug-16, Volume: 39, Issue:17, 1996
Stereoisomers of ketoconazole: preparation and biological activity.Journal of medicinal chemistry, , Jul-24, Volume: 35, Issue:15, 1992
Mechanism and inhibition of cytochrome P-450 aromatase.Journal of medicinal chemistry, , Volume: 33, Issue:11, 1990
Synthesis of novel thiazolyl hydrazone derivatives as potent dual monoamine oxidase-aromatase inhibitors.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
An overview on Estrogen receptors signaling and its ligands in breast cancer.European journal of medicinal chemistry, , Nov-05, Volume: 241, 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, , Oct-05, Volume: 240, 2022
Isoxazole derivatives as anticancer agent: A review on synthetic strategies, mechanism of action and SAR studies.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
Diterpenoids with Aromatase Inhibitory Activity from the Rhizomes of Journal of natural products, , 06-25, Volume: 84, Issue:6, 2021
Balanced dual acting compounds targeting aromatase and estrogen receptor α as an emerging therapeutic opportunity to counteract estrogen responsive breast cancer.European journal of medicinal chemistry, , Nov-15, Volume: 224, 2021
Synthesis, biological evaluation, and docking study of indole aryl sulfonamides as aromatase inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
Targeting Orthosteric and Allosteric Pockets of Aromatase via Dual-Mode Novel Azole Inhibitors.ACS medicinal chemistry letters, , May-14, Volume: 11, Issue:5, 2020
Synthesis, molecular docking, and QSAR study of bis-sulfonamide derivatives as potential aromatase inhibitors.Bioorganic & medicinal chemistry, , 10-01, Volume: 27, Issue:19, 2019
Rational design of allosteric modulators of the aromatase enzyme: An unprecedented therapeutic strategy to fight breast cancer.European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
Synthesis, molecular docking, and QSAR study of sulfonamide-based indoles as aromatase inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Potent aromatase inhibitors and molecular mechanism of inhibitory action.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Aromatase inhibitors and apoptotic inducers: Design, synthesis, anticancer activity and molecular modeling studies of novel phenothiazine derivatives carrying sulfonamide moiety as hybrid molecules.European journal of medicinal chemistry, , Jul-07, Volume: 134, 2017
Structure-activity relationships and docking studies of synthetic 2-arylindole derivatives determined with aromatase and quinone reductase 1.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 27, Issue:24, 2017
A new Suzuki synthesis of triphenylethylenes that inhibit aromatase and bind to estrogen receptors α and β.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Synthesis and aromatase inhibitory evaluation of 4-N-nitrophenyl substituted amino-4H-1,2,4-triazole derivatives.Bioorganic & medicinal chemistry, , 10-01, Volume: 24, Issue:19, 2016
[no title available]European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Synthesis and biological characterization of 3-(imidazol-1-ylmethyl)piperidine sulfonamides as aromatase inhibitors.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 26, Issue:13, 2016
Synthesis, biological evaluation, and molecular docking studies of new pyrazol-3-one derivatives with aromatase inhibition activities.Chemical biology & drug design, , Volume: 88, Issue:6, 2016
Synthesis and molecular docking of 1,2,3-triazole-based sulfonamides as aromatase inhibitors.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities.Journal of medicinal chemistry, , Mar-26, Volume: 58, Issue:6, 2015
Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health.Journal of medicinal chemistry, , Oct-08, Volume: 58, Issue:19, 2015
Investigation of fluorinated and bifunctionalized 3-phenylchroman-4-one (isoflavanone) aromatase inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 22, Issue:1, 2014
Design, synthesis, and structure-activity relationships of azolylmethylpyrroloquinolines as nonsteroidal aromatase inhibitors.Journal of medicinal chemistry, , Oct-10, Volume: 56, Issue:19, 2013
Design, synthesis and aromatase inhibitory activities of novel indole-imidazole derivatives.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Tetrahydropyrroloquinolinone type dual inhibitors of aromatase/aldosterone synthase as a novel strategy for breast cancer patients with elevated cardiovascular risks.Journal of medicinal chemistry, , Jan-24, Volume: 56, Issue:2, 2013
New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 22, Issue:5, 2012
Novel aromatase inhibitors by structure-guided design.Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrol.Bioorganic & medicinal chemistry, , Apr-01, Volume: 20, Issue:7, 2012
Structure-based design of potent aromatase inhibitors by high-throughput docking.Journal of medicinal chemistry, , Jun-23, Volume: 54, Issue:12, 2011
Lead optimization of 4-imidazolylflavans: new promising aromatase inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
Synthesis and structure-activity relationship of 1- and 2-substituted-1,2,3-triazole letrozole-based analogues as aromatase inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.Journal of medicinal chemistry, , Jan-08, Volume: 52, Issue:1, 2009
Synthesis of 6- or 4-functionalized indoles via a reductive cyclization approach and evaluation as aromatase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 2008
Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Synthesis and biological evaluation of 4-imidazolylflavans as nonsteroidal aromatase inhibitors.Bioorganic chemistry, , Volume: 32, Issue:6, 2004
Novel sulfonanilide analogs decrease aromatase activity in breast cancer cells: synthesis, biological evaluation, and ligand-based pharmacophore identification.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Novel sulfonanilide analogues suppress aromatase expression and activity in breast cancer cells independent of COX-2 inhibition.Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
Developing steroidal aromatase inhibitors-an effective armament to win the battle against breast cancer.European journal of medicinal chemistry, , Nov-13, Volume: 105, 2015
Development of a new class of aromatase inhibitors: design, synthesis and inhibitory activity of 3-phenylchroman-4-one (isoflavanone) derivatives.Bioorganic & medicinal chemistry, , Apr-15, Volume: 20, Issue:8, 2012
Structure-activity relationships of new A,D-ring modified steroids as aromatase inhibitors: design, synthesis, and biological activity evaluation.Journal of medicinal chemistry, , Oct-06, Volume: 48, Issue:20, 2005
Synthesis of androst-5-en-7-ones and androsta-3,5-dien-7-ones and their related 7-deoxy analogs as conformational and catalytic probes for the active site of aromatase.Journal of medicinal chemistry, , Jul-08, Volume: 37, Issue:14, 1994
Mechanism and inhibition of cytochrome P-450 aromatase.Journal of medicinal chemistry, , Volume: 33, Issue:11, 1990
Interactions of thiol-containing androgens with human placental aromatase.Journal of medicinal chemistry, , Volume: 32, Issue:1, 1989
Recent developments in steroidal and nonsteroidal aromatase inhibitors for the chemoprevention of estrogen-dependent breast cancer.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Investigation of fluorinated and bifunctionalized 3-phenylchroman-4-one (isoflavanone) aromatase inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 22, Issue:1, 2014
New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
New aromatase inhibitors. Synthesis and inhibitory activity of pyridinyl-substituted flavanone derivatives.Bioorganic & medicinal chemistry letters, , Apr-08, Volume: 12, Issue:7, 2002
Recent developments in steroidal and nonsteroidal aromatase inhibitors for the chemoprevention of estrogen-dependent breast cancer.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Investigation of fluorinated and bifunctionalized 3-phenylchroman-4-one (isoflavanone) aromatase inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 22, Issue:1, 2014
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
An overview on Estrogen receptors signaling and its ligands in breast cancer.European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
Recent Progress in the Discovery of Next Generation Inhibitors of Aromatase from the Structure-Function Perspective.Journal of medicinal chemistry, , 06-09, Volume: 59, Issue:11, 2016
Developing steroidal aromatase inhibitors-an effective armament to win the battle against breast cancer.European journal of medicinal chemistry, , Nov-13, Volume: 105, 2015
Inhibitory effect of Rhus verniciflua Stokes extract on human aromatase activity; butin is its major bioactive component.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 24, Issue:7, 2014
Synthesis and bioconversions of formestane.Journal of natural products, , Oct-25, Volume: 76, Issue:10, 2013
New structure-activity relationships of A- and D-ring modified steroidal aromatase inhibitors: design, synthesis, and biochemical evaluation.Journal of medicinal chemistry, , Apr-26, Volume: 55, Issue:8, 2012
Novel aromatase inhibitors by structure-guided design.Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Molecular docking and QSAR study on steroidal compounds as aromatase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:12, 2010
An efficient steroid pharmacophore-based strategy to identify new aromatase inhibitors.European journal of medicinal chemistry, , Volume: 44, Issue:10, 2009
Evaluation of ursolic acid isolated from Ilex paraguariensis and derivatives on aromatase inhibition.European journal of medicinal chemistry, , Volume: 43, Issue:9, 2008
Structure-activity relationships of new A,D-ring modified steroids as aromatase inhibitors: design, synthesis, and biological activity evaluation.Journal of medicinal chemistry, , Oct-06, Volume: 48, Issue:20, 2005
Synthesis and evaluation of a new series of mechanism-based aromatase inhibitors.Journal of medicinal chemistry, , May-01, Volume: 35, Issue:9, 1992
Synthesis and biochemical studies of 16- or 19-substituted androst-4-enes as aromatase inhibitors.Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Mechanism and inhibition of cytochrome P-450 aromatase.Journal of medicinal chemistry, , Volume: 33, Issue:11, 1990
Interactions of thiol-containing androgens with human placental aromatase.Journal of medicinal chemistry, , Volume: 32, Issue:1, 1989
Synthesis and evaluation of 4-(substituted thio)-4-androstene-3,17-dione derivatives as potential aromatase inhibitors.Journal of medicinal chemistry, , Volume: 29, Issue:4, 1986
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
Mechanism and inhibition of cytochrome P-450 aromatase.Journal of medicinal chemistry, , Volume: 33, Issue:11, 1990
Developing steroidal aromatase inhibitors-an effective armament to win the battle against breast cancer.European journal of medicinal chemistry, , Nov-13, Volume: 105, 2015
Time-dependent inactivation of aromatase by 6-alkylandrosta-1,4-diene-3,17-diones. Effects of length and configuration of 6-alkyl group.Journal of medicinal chemistry, , Mar-01, Volume: 39, Issue:5, 1996
Mechanism and inhibition of cytochrome P-450 aromatase.Journal of medicinal chemistry, , Volume: 33, Issue:11, 1990
Effects of steroid D-ring modification on suicide inactivation and competitive inhibition of aromatase by analogues of androsta-1,4-diene-3,17-dione.Journal of medicinal chemistry, , Volume: 32, Issue:3, 1989
Crystallographic and molecular modeling studies on 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione and its butyl analogue, inhibitors of mammalian aromatase. Comparison with natural substrates: prediction of enantioselectivity for N-alkyl derivatives.Journal of medicinal chemistry, , Volume: 33, Issue:9, 1990
Analogues of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents.Journal of medicinal chemistry, , Volume: 30, Issue:9, 1987
Analogues of aminoglutethimide: selective inhibition of aromatase.Journal of medicinal chemistry, , Volume: 28, Issue:2, 1985
An overview on Estrogen receptors signaling and its ligands in breast cancer.European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
Recent Progress in the Discovery of Next Generation Inhibitors of Aromatase from the Structure-Function Perspective.Journal of medicinal chemistry, , 06-09, Volume: 59, Issue:11, 2016
Heteroatom insertion into 3,4-dihydro-1H-quinolin-2-ones leads to potent and selective inhibitors of human and rat aldosterone synthase.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Modulation of cytochromes P450 with xanthone-based molecules: from aromatase to aldosterone synthase and steroid 11β-hydroxylase inhibition.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
Tetrahydropyrroloquinolinone type dual inhibitors of aromatase/aldosterone synthase as a novel strategy for breast cancer patients with elevated cardiovascular risks.Journal of medicinal chemistry, , Jan-24, Volume: 56, Issue:2, 2013
Selective dual inhibitors of CYP19 and CYP11B2: targeting cardiovascular diseases hiding in the shadow of breast cancer.Journal of medicinal chemistry, , Aug-23, Volume: 55, Issue:16, 2012
Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrol.Bioorganic & medicinal chemistry, , Apr-01, Volume: 20, Issue:7, 2012
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.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
N-(Pyridin-3-yl)benzamides as selective inhibitors of human aldosterone synthase (CYP11B2).Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Fine-tuning the selectivity of aldosterone synthase inhibitors: structure-activity and structure-selectivity insights from studies of heteroaryl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-one derivatives.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
Design, synthesis, and biological evaluation of imidazolyl derivatives of 4,7-disubstituted coumarins as aromatase inhibitors selective over 17-α-hydroxylase/C17-20 lyase.Journal of medicinal chemistry, , Mar-24, Volume: 54, Issue:6, 2011
Novel highly potent and selective nonsteroidal aromatase inhibitors: synthesis, biological evaluation and structure-activity relationships investigation.Journal of medicinal chemistry, , Jul-22, Volume: 53, Issue:14, 2010
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
CYP19 (aromatase): exploring the scaffold flexibility for novel selective inhibitors.Bioorganic & medicinal chemistry, , Sep-15, Volume: 16, Issue:18, 2008
Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Imidazolylmethylbenzophenones as highly potent aromatase inhibitors.Journal of medicinal chemistry, , Jul-26, Volume: 50, Issue:15, 2007
Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase.Journal of medicinal chemistry, , Mar-01, Volume: 44, Issue:5, 2001
Design and synthesis of a new type of non steroidal human aromatase inhibitors.Bioorganic & medicinal chemistry letters, , May-05, Volume: 8, Issue:9, 1998
Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.Journal of medicinal chemistry, , Volume: 34, Issue:2, 1991
Mechanism and inhibition of cytochrome P-450 aromatase.Journal of medicinal chemistry, , Volume: 33, Issue:11, 1990
An overview on Estrogen receptors signaling and its ligands in breast cancer.European journal of medicinal chemistry, , Nov-05, Volume: 241, 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, , Oct-05, Volume: 240, 2022
Diterpenoids with Aromatase Inhibitory Activity from the Rhizomes of Journal of natural products, , 06-25, Volume: 84, Issue:6, 2021
Evaluation of synthesized coumarin derivatives on aromatase inhibitory activity.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 27, Issue:12, 2017
Developing steroidal aromatase inhibitors-an effective armament to win the battle against breast cancer.European journal of medicinal chemistry, , Nov-13, Volume: 105, 2015
Exemestane metabolites: Synthesis, stereochemical elucidation, biochemical activity and anti-proliferative effects in a hormone-dependent breast cancer cell line.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Novel aromatase inhibitors by structure-guided design.Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Synthesis of Triphenylethylene Bisphenols as Aromatase Inhibitors That Also Modulate Estrogen Receptors.Journal of medicinal chemistry, , Jan-14, Volume: 59, Issue:1, 2016
A new Suzuki synthesis of triphenylethylenes that inhibit aromatase and bind to estrogen receptors α and β.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Synthesis of mixed (E,Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Screening of herbal constituents for aromatase inhibitory activity.Bioorganic & medicinal chemistry, , Sep-15, Volume: 16, Issue:18, 2008
New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
Synthesis, structure elucidation, and biochemical evaluation of 7 alpha- and 7 beta-arylaliphatic-substituted androst-4-ene-3,17-diones as inhibitors of aromatase.Journal of medicinal chemistry, , Jul-21, Volume: 38, Issue:15, 1995
Synthesis and biochemical evaluation of inhibitors of estrogen biosynthesis.Journal of medicinal chemistry, , Volume: 21, Issue:10, 1978
Developing steroidal aromatase inhibitors-an effective armament to win the battle against breast cancer.European journal of medicinal chemistry, , Nov-13, Volume: 105, 2015
Molecular docking and QSAR study on steroidal compounds as aromatase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:12, 2010
Role of hydrophilic interaction in binding of hydroxylated 3-deoxy C(19) steroids to the active site of aromatase.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Synthesis and biochemical studies of 16- or 19-substituted androst-4-enes as aromatase inhibitors.Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Modulation of cytochromes P450 with xanthone-based molecules: from aromatase to aldosterone synthase and steroid 11β-hydroxylase inhibition.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
Novel steroidal inhibitors of human cytochrome P45017 alpha (17 alpha-hydroxylase-C17,20-lyase): potential agents for the treatment of prostatic cancer.Journal of medicinal chemistry, , Jun-23, Volume: 38, Issue:13, 1995
Hybrid dual aromatase-steroid sulfatase inhibitors with exquisite picomolar inhibitory activity.ACS medicinal chemistry letters, , Mar-10, Volume: 2, Issue:3, 2011
Dual aromatase-steroid sulfatase inhibitors.Journal of medicinal chemistry, , Jul-26, Volume: 50, Issue:15, 2007
First dual aromatase-steroid sulfatase inhibitors.Journal of medicinal chemistry, , Jul-17, Volume: 46, Issue:15, 2003
Recent developments of C-4 substituted coumarin derivatives as anticancer agents.European journal of medicinal chemistry, , Aug-25, Volume: 119, 2016
Spongiapyridine and related spongians isolated from an Indonesian Spongia sp.Journal of natural products, , Jul-25, Volume: 77, Issue:7, 2014
Chemopreventive and antioxidant activity of 6-substituted imidazo[2,1-b]thiazoles.European journal of medicinal chemistry, , Volume: 68, 2013
Synthesis and bioconversions of formestane.Journal of natural products, , Oct-25, Volume: 76, Issue:10, 2013
Optimizing thiadiazole analogues of resveratrol versus three chemopreventive targets.Bioorganic & medicinal chemistry, , Jan-01, Volume: 20, Issue:1, 2012
Optimization of thiazole analogues of resveratrol for induction of NAD(P)H:quinone reductase 1 (QR1).Bioorganic & medicinal chemistry, , Dec-15, Volume: 20, Issue:24, 2012
Design, synthesis, and biological evaluation of callophycin A and analogues as potential chemopreventive and anticancer agents.Bioorganic & medicinal chemistry, , Nov-01, Volume: 19, Issue:21, 2011
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Aromatase inhibitors from Broussonetia papyrifera.Journal of natural products, , Volume: 64, Issue:10, 2001
Synthesis, structure-activity relationships and molecular docking studies of phenyldiazenyl sulfonamides as aromatase inhibitors.European journal of medicinal chemistry, , Nov-15, Volume: 224, 2021
Studies on non-steroidal inhibitors of aromatase enzyme; 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl)thiazole derivatives.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Optimizing thiadiazole analogues of resveratrol versus three chemopreventive targets.Bioorganic & medicinal chemistry, , Jan-01, Volume: 20, Issue:1, 2012
Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrol.Bioorganic & medicinal chemistry, , Apr-01, Volume: 20, Issue:7, 2012
Optimization of thiazole analogues of resveratrol for induction of NAD(P)H:quinone reductase 1 (QR1).Bioorganic & medicinal chemistry, , Dec-15, Volume: 20, Issue:24, 2012
Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities.Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009
Diterpenoids with Aromatase Inhibitory Activity from the Rhizomes of Journal of natural products, , 06-25, Volume: 84, Issue:6, 2021
Studies on non-steroidal inhibitors of aromatase enzyme; 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl)thiazole derivatives.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Synthesis, molecular docking, and QSAR study of sulfonamide-based indoles as aromatase inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Design and synthesis of functionalized piperazin-1yl-(E)-stilbenes as inhibitors of 17α-hydroxylase-C17,20-lyase (Cyp17).Bioorganic & medicinal chemistry letters, , 07-15, Volume: 28, Issue:13, 2018
Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Synthesis and structure-activity relationship of 1- and 2-substituted-1,2,3-triazole letrozole-based analogues as aromatase inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Synthesis and biochemical evaluation of a range of sulfonated derivatives of 4-hydroxybenzyl imidazole as highly potent inhibitors of rat testicular 17alpha-hydroxylase/17,20-lyase (P-450(17alpha)).Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.Journal of medicinal chemistry, , Volume: 34, Issue:2, 1991
Recent developments in steroidal and nonsteroidal aromatase inhibitors for the chemoprevention of estrogen-dependent breast cancer.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Development of a new class of aromatase inhibitors: design, synthesis and inhibitory activity of 3-phenylchroman-4-one (isoflavanone) derivatives.Bioorganic & medicinal chemistry, , Apr-15, Volume: 20, Issue:8, 2012
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Synthesis and characterization of azole isoflavone inhibitors of aromatase.Bioorganic & medicinal chemistry, , Jun-02, Volume: 13, Issue:12, 2005
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.Journal of medicinal chemistry, , Jul-29, Volume: 47, Issue:16, 2004
Recent developments in steroidal and nonsteroidal aromatase inhibitors for the chemoprevention of estrogen-dependent breast cancer.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Evaluation of ursolic acid isolated from Ilex paraguariensis and derivatives on aromatase inhibition.European journal of medicinal chemistry, , Volume: 43, Issue:9, 2008
Screening of herbal constituents for aromatase inhibitory activity.Bioorganic & medicinal chemistry, , Sep-15, Volume: 16, Issue:18, 2008
Screening of herbal constituents for aromatase inhibitory activity.Bioorganic & medicinal chemistry, , Sep-15, Volume: 16, Issue:18, 2008
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.Journal of medicinal chemistry, , Jul-29, Volume: 47, Issue:16, 2004
Recent developments in steroidal and nonsteroidal aromatase inhibitors for the chemoprevention of estrogen-dependent breast cancer.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Development of a new class of aromatase inhibitors: design, synthesis and inhibitory activity of 3-phenylchroman-4-one (isoflavanone) derivatives.Bioorganic & medicinal chemistry, , Apr-15, Volume: 20, Issue:8, 2012
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.Journal of medicinal chemistry, , Jul-29, Volume: 47, Issue:16, 2004
[no title available]European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Evaluation of 7-hydroxy-flavones as inhibitors of oestrone and oestradiol biosynthesis.Journal of enzyme inhibition, , Volume: 16, Issue:5, 2001
Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health.Journal of medicinal chemistry, , Oct-08, Volume: 58, Issue:19, 2015
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase.Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
Interactions of thiol-containing androgens with human placental aromatase.Journal of medicinal chemistry, , Volume: 32, Issue:1, 1989
Is there a case for P-450 inhibitors in cancer treatment?Journal of medicinal chemistry, , Volume: 32, Issue:10, 1989
Balanced dual acting compounds targeting aromatase and estrogen receptor α as an emerging therapeutic opportunity to counteract estrogen responsive breast cancer.European journal of medicinal chemistry, , Nov-15, Volume: 224, 2021
Rational design of allosteric modulators of the aromatase enzyme: An unprecedented therapeutic strategy to fight breast cancer.European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
Recent Progress in the Discovery of Next Generation Inhibitors of Aromatase from the Structure-Function Perspective.Journal of medicinal chemistry, , 06-09, Volume: 59, Issue:11, 2016
Synthesis of mixed (E,Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Dihydrobenzisoxazole-4-one compounds are novel selective inhibitors of aldosterone synthase (CYP11B2) with in vivo activity.Bioorganic & medicinal chemistry letters, , 03-01, Volume: 28, Issue:5, 2018
Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.ACS medicinal chemistry letters, , Dec-12, Volume: 4, Issue:12, 2013
Enables
This protein enables 7 target(s):
| Target | Category | Definition |
|---|
| iron ion binding | molecular function | Binding to an iron (Fe) ion. [GOC:ai] |
| steroid hydroxylase activity | molecular function | Catalysis of the formation of a hydroxyl group on a steroid by incorporation of oxygen from O2. [ISBN:0721662544] |
| electron transfer activity | molecular function | A molecular function representing the directed movement of electrons from one molecular entity to another, typically mediated by electron carriers or acceptors, resulting in the transfer of energy and/or the reduction-oxidation (redox) transformation of chemical species. This activity is fundamental to various biological processes, including cellular respiration and photosynthesis, as well as numerous enzymatic reactions involved in metabolic pathways. [Wikipedia:Electron_transfer] |
| oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen | molecular function | Catalysis of an oxidation-reduction (redox) reaction in which hydrogen or electrons are transferred from reduced flavin or flavoprotein and one other donor, and one atom of oxygen is incorporated into one donor. [GOC:mah] |
| oxygen binding | molecular function | Binding to oxygen (O2). [GOC:jl] |
| heme binding | molecular function | Binding to a heme, a compound composed of iron complexed in a porphyrin (tetrapyrrole) ring. [GOC:ai] |
| aromatase activity | molecular function | Catalysis of the reduction of an aliphatic ring to yield an aromatic ring. [GOC:cb] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
Involved In
This protein is involved in 15 target(s):
| Target | Category | Definition |
|---|
| negative regulation of chronic inflammatory response | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of a chronic inflammatory response. [GOC:add] |
| steroid biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of steroids, compounds with a 1,2,cyclopentanoperhydrophenanthrene nucleus; includes de novo formation and steroid interconversion by modification. [GOC:go_curators] |
| estrogen biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of estrogens, C18 steroid hormones that can stimulate the development of female sexual characteristics. Also found in plants. [ISBN:0198506732] |
| androgen catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of androgens, C19 steroid hormones that can stimulate the development of male sexual characteristics. [ISBN:0198506732] |
| syncytium formation | biological process | The formation of a syncytium, a mass of cytoplasm containing several nuclei enclosed within a single plasma membrane. Syncytia are normally derived from single cells that fuse or fail to complete cell division. [ISBN:0198506732] |
| negative regulation of macrophage chemotaxis | biological process | Any process that decreases the rate, frequency or extent of macrophage chemotaxis. Macrophage chemotaxis is the movement of a macrophage in response to an external stimulus. [GOC:BHF, GOC:dph, GOC:tb] |
| sterol metabolic process | biological process | The chemical reactions and pathways involving sterols, steroids with one or more hydroxyl groups and a hydrocarbon side-chain in the molecule. [ISBN:0198547684] |
| female genitalia development | biological process | The process whose specific outcome is the progression of the female genitalia over time, from formation to the mature structure. [GOC:mah] |
| mammary gland development | biological process | The process whose specific outcome is the progression of the mammary gland over time, from its formation to the mature structure. The mammary gland is a large compound sebaceous gland that in female mammals is modified to secrete milk. Its development starts with the formation of the mammary line and ends as the mature gland cycles between nursing and weaning stages. [PMID:9576833] |
| uterus development | biological process | The reproductive developmental process whose specific outcome is the progression of the uterus over time, from its formation to the mature structure. [GOC:dph, GOC:ebc] |
| prostate gland growth | biological process | The increase in size or mass of the prostate gland where the increase in size or mass has the specific outcome of the progression of the gland, from its formation to its mature state. [GOC:dph] |
| testosterone biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of testosterone, an androgen having 17beta-hydroxy and 3-oxo groups, together with unsaturation at C-4 C-5. [GOC:dph, GOC:yaf] |
| positive regulation of estradiol secretion | biological process | Any process that activates or increases the frequency, rate or extent of estradiol secretion. [GOC:sl] |
| female gonad development | biological process | The process whose specific outcome is the progression of the female gonad over time, from its formation to the mature structure. [GOC:dph, GOC:jid, GOC:tb] |
| response to estradiol | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of stimulus by estradiol, a C18 steroid hormone hydroxylated at C3 and C17 that acts as a potent estrogen. [GOC:mah, ISBN:0911910123] |