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

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Feau C, Arnold LA, Kosinski A, Zhu F, Connelly M, Guy RK

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

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

PubMed ID
19645433 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
BicalutamideAndrogen receptorIC 50 (nM)120007.223Details
Flufenamic acidAndrogen receptorEC 50 (nM)670007.223Details