Article
Syntheses and potential anti-prostate cancer activities of ionone-based chalcones.
Bioorganic & medicinal chemistry letters - 15 Feb 2009
Zhou Jinming, Geng Guoyan, Batist Gerald, Wu Jian Hui
Abstract excerpt
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 IC(50) value of 0.74 microM in LNCaP cells potently antagonizes DHT-induced transactivation of the wild type and the clinically relevant T877A, W741C and H874Y mutated androgen receptors, representing...
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