Discovery and biological characterization of a novel series of androgen receptor modulators.

ABSTRACT:

Background and purpose

Selective androgen receptor modulators are of great value in the treatment of prostate cancer. The purpose of this study was to provide a preliminary characterization of a new class of non-steroidal androgen receptor modulators discovered in a high-throughput screening campaign.

Experimental approach

Competitive receptor binding, luciferase-based reporter methods, cell proliferation and in vivo assays were employed to evaluate an initial set of compounds from chemistry efforts.

Key results

Forty-nine analogues from the chemistry efforts showed high affinity binding to androgen receptors, agonist and/or antagonist activities in both CV-1 and MDA-MB-453 transfection assays. A proliferation assay in LNCaP cells also exhibited this profile. A repres

SUBMITTER: Zhou C 

PROVIDER: S-EPMC2442451 | biostudies-literature | 2008 May

REPOSITORIES: biostudies-literature