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

High throughput cell-based screening led to the identification of 3-aryloxy lactams as potent androgen receptor (AR) antagonists. Refinement of these leads to improve the ADME profile and remove residual agonism led to the discovery of 12, a potent full antagonist with greater oral bioavailability. Improvements in the ADME profile were realized by designing more ligand-efficient molecules with reduced molecular weights and lower lipophilicities.

 

Written by:
Guo C, Kephart S, Ornelas M, Gonzalez J, Linton A, Pairish M, Nagata A, Greasley S, Elleraas J, Hosea N, Engebretsen J, Fanjul AN.   Are you the author?
Oncology Medicinal Chemistry, Pfizer Worldwide Research & Development, San Diego, CA 92121, USA.

Reference: Bioorg Med Chem Lett. 2012 Jan 15;22(2):1230-6.
doi: 10.1016/j.bmcl.2011.11.068

PubMed Abstract
PMID: 22197140

UroToday.com Investigational Urology Section