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

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.

SUBMITTER: Feau C

PROVIDER: S-EPMC2763043 | biostudies-literature | 2009 Oct

REPOSITORIES: biostudies-literature

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

Féau Clémentine C Arnold Leggy A LA Kosinski Aaron A Zhu Fangyi F Connelly Michele M Guy R Kiplin RK

ACS chemical biology 20091001 10

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 hor ...[more]

PMID: 19645433

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