Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC).
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.
Jung
Michael E
ME
Department of Chemistry and Biochemistry, University of California, Los Angeles, California 90095, USA. jung@chem.ucla.edu
Ouk
Samedy
S
Yoo
Dongwon
D
Sawyers
Charles L
CL
Chen
Charlie
C
Tran
Chris
C
Wongvipat
John
J
D059002:Androgen Receptor Antagonists; D000728:Androgens; D000818:Animals; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D008297:Male; D009919:Orchiectomy; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology / Q000601:surgery*; D011944:Receptors, Androgen / Q000378:metabolism; D013329:Structure-Activity Relationship; D013867:Thiohydantoins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D047368:Tumor Burden / Q000187:drug effects; D023041:Xenograft Model Antitumor Assays
D059002:Androgen Receptor Antagonists; D000728:Androgens; D011944:Receptors, Androgen; D013867:Thiohydantoins