Novel Flufenamic Acid Analogues as Inhibitors of Androgen Receptor Mediated Transcription
ACS Chemical Biology2009Vol. 4(10), pp. 834–843
Citations Over TimeTop 12% of 2009 papers
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.
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