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Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 2, 2012, Pages 1230-1236

Discovery of 3-aryloxy-lactam analogs as potent androgen receptor full antagonists for treating castration resistant prostate cancer

(12) Guo, Chuangxing a Kephart, Susan a Ornelas, Martha a Gonzalez, Javier a Linton, Angelica a Pairish, Mason a Nagata, Asako a Greasley, Samantha a Elleraas, Jeff a Hosea, Natilie a Engebretsen, Jon a Fanjul, Andrea N a

a PFIZER INC (United States)

Author keywords

Androgen receptor; AR antagonist; Castration resistant prostate cancer; CRPC; LBD; Ligand efficiency; NHR; Polar surface area; Prostate cancer; PSA

Indexed keywords

3 ARYLOXY LACTAM DERIVATIVE; 4 [3 [4 CYANO 3 (TRIFLUOROMETHYL)PHENYL] 5,5 DIMETHYL 4 OXO 2 THIOXO 1 IMIDAZOLIDINYL] 2 FLUORO N METHYLBENZAMIDE; ANDROGEN RECEPTOR ANTAGONIST; BICALUTAMIDE; BMS 641988; UNCLASSIFIED DRUG;

ARTICLE; BIOAVAILABILITY; CASTRATION RESISTANT PROSTATE CANCER; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG ABSORPTION; DRUG ANTAGONISM; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG IDENTIFICATION; DRUG PENETRATION; DRUG SOLUBILITY; HIGH THROUGHPUT SCREENING; IC 50; LIPOPHILICITY; MOLECULAR WEIGHT; NONHUMAN; RAT;

DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; LACTAMS; MALE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROSTATIC NEOPLASMS; RECEPTORS, ANDROGEN; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84855679381 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2011.11.068 Document Type: Article

Times cited : (11)

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