Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC) Journal Article
| Authors: | Jung, M. E.; Ouk, S.; Yoo, D.; Sawyers, C. L.; Chen, C.; Tran, C.; Wongvipat, J. |
| Article Title: | Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC) |
| Abstract: | A structure-activity relationship study was carried out on a series of thiohydantoins and their analogues 14 which led to the discovery of 92 (MDV3100) as the clinical candidate for the treatment of hormone refractory prostate cancer. © 2010 American Chemical Society. |
| Keywords: | controlled study; unclassified drug; human cell; nonhuman; animals; animal experiment; drug structure; drug effect; dose-response relationship, drug; xenograft model antitumor assays; cell line, tumor; drug synthesis; structure activity relation; structure-activity relationship; prostate cancer; prostatic neoplasms; gene expression regulation, neoplastic; tumor burden; androgen receptor; drug blood level; bicalutamide; flutamide; mdv 3100; nilutamide; castration; orchiectomy; receptors, androgen; concentration response; ru 59063; thiohydantoin derivative; 1,4 diazidobutane; 2 (4 azidobutylamino) 2 methylpropionitrile; 2 (4 hydroxyphenylamino) 2 methylpropanenitrile; 2 methyl 2 (4 methylphenyl)aminopropane nitrile; 2 methyl 2 phenylaminopropanenitrile; 4 [3 (3 azidopropyl) 4,4 dimethyl 5 oxo 2 thioxoimidazolidin 1 yl] 2 trifluoromethylbenzonitrile; 4 [3 (4 azidobutyl) 4,4 dimethyl 5 oxo 2 thioxoimidazolidin 1 yl] 2 trifluoromethylbenzonitrile; 4 [3 (4 azidobutyl) 5 imino 4,4 dimethyl 2 thioxoimidazolidin 1 yl] 2 trifluoromethylbenzonitrile; 4 [3 (4 hydroxyphenyl) 4,4 dimethyl 5 oxo 2 thioxoimidazolidin 1 yl] 2 trifluoromethylbenzonitrile; 4 [3 (4 hydroxyphenyl) 5 imino 4,4 dimethyl 2 thioxoimidazolidin 1 yl] 2 trifluoromethylbenzonitrile; 4 [3 (4 methylphenyl) 4 ethyl 5 oxo 2 thioxoimidazolidin 1 yl] 2 trifluoromethylbenzonitrile; 4 [3 (4 methylphenyl) 4 methyl 5 oxo 2 thioxoimidazolidin 1 yl] 2 trifluoromethylbenzonitrile; 4 [3 (4 methylphenyl) 4,4 dimethyl 5 oxo 2 thioxoimidazolidin 1 yl] 2 trifluoromethylbenzonitrile; 4 [3 (4 methylphenyl) 5 oxo 2 thioxoimidazolidin 1 yl] 2 trifluoromethylbenzonitrile; 4 [3 (5 azidopentyl) 4,4 dimethyl 5 oxo 2 thioxoimidazolidin 1 yl] 2 trifluoromethylbenzonitrile; 4 [3 (6 azidohexyl) 4,4 dimethyl 5 oxo 2 thioxoimidazolidin 1 yl] 2 trifluoromethylbenzonitrile; 4 [3 (7 azidoheptyl) 4,4 dimethyl 5 oxo 2 thioxoimidazolidin 1 yl] 2 trifluoromethylbenzonitrile; 4 [3 phenyl 4,4 dimethyl 5 oxo 2 thioxoimidazolidin 1 yl] 2 trifluoromethylbenzonitrile; 4 azidobutylamine; 4 isothiocyanato 2 trifluoromethylbenzonitrile; hormone antagonist; hydroxyflutamide; n(4 cyano 3 trifluoromethylphenyl) n' (4 methylphenyl)thiourea; thiohydantoins |
| Journal Title: | Journal of Medicinal Chemistry |
| Volume: | 53 |
| Issue: | 7 |
| ISSN: | 0022-2623 |
| Publisher: | American Chemical Society |
| Date Published: | 2010-04-08 |
| Start Page: | 2779 |
| End Page: | 2796 |
| Language: | English |
| DOI: | 10.1021/jm901488g |
| PUBMED: | 20218717 |
| PROVIDER: | scopus |
| PMCID: | PMC3180999 |
| DOI/URL: | |
| Notes: | --- - "Cited By (since 1996): 1" - "Export Date: 20 April 2011" - "CODEN: JMCMA" - "Source: Scopus" |
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