Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 4, Pages 1183-1186Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.12.089
Keywords
Androgen receptor; Mutation; Antiandrogen; Pan-antagonist; Ionone derivatives
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Funding
- Canadian Institute of Health Research (CIHR) [MOP-74741]
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We report the SAR studies of 43 ionone-based chalcones that demonstrate substantial in vitro anti-proliferative activities in LNCaP, MDA-PCa-2b, 22Rv1, C4-2B and PC-3 prostate cancer cell lines. Compound 25 with an IC50 value of 0.74 mu M in LNCaP cells potently antagonizes DHT-induced transactivation of the wild type and the clinically relevant T877A, W741C and H874Y mutated androgen receptors, representing a novel chalcone as pan-antagonist of androgen receptor. (C) 2008 Elsevier Ltd. All rights reserved.
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