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ACS Chem Biol. 2009 Oct 16;4(10):834-43. doi: 10.1021/cb900143a.

Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription.

Author information

1
Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, USA.

Abstract

The androgen receptor (AR), which mediates the signals of androgens, plays a crucial role in prostate-related diseases. Although widely used, currently marketed anti-androgenic drugs have significant side effects. Several studies have revealed that non-steroidal anti-inflammatory drugs, such as flufenamic acid, block AR transcriptional activity. Herein we describe the development of small molecule analogues of flufenamic acid that antagonize AR. This novel class of AR inhibitors binds to the hormone binding site, blocks AR transcription activity, and acts on AR target genes.

PMID:
19645433
PMCID:
PMC2763043
DOI:
10.1021/cb900143a
[Indexed for MEDLINE]
Free PMC Article

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