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.

• Authors: Michael E Jung, Samedy Ouk, Dongwon Yoo, Charles L Sawyers, Charlie Chen, Chris Tran, John Wongvipat
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 53 Issue 7 Pg. 2779-96 (Apr 08 2010) ISSN: 1520-4804 [Electronic] United States
• PMID: 20218717 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)

Chemical References

• Androgen Receptor Antagonists
• Androgens
• Receptors, Androgen
• Thiohydantoins

Topics

• Androgen Receptor Antagonists
• Androgens
• Animals
• Cell Line, Tumor
• Dose-Response Relationship, Drug
• Gene Expression Regulation, Neoplastic (drug effects)
• Male
• Orchiectomy
• Prostatic Neoplasms (drug therapy, genetics, pathology, surgery)
• Receptors, Androgen (metabolism)
• Structure-Activity Relationship
• Thiohydantoins (chemical synthesis, chemistry, pharmacology, therapeutic use)
• Tumor Burden (drug effects)
• Xenograft Model Antitumor Assays