Article
Design and synthesis of androgen receptor antagonists with bulky side chains for overcoming antiandrogen resistance.
Journal of medicinal chemistry - 10 Sept 2009
Zhou Jinming, Geng Guoyan, Shi Qingwen, Sauriol Francoise, Wu Jian Hui
Abstract excerpt
Incorporation of curcumin and beta-ionone into one chemical entity led to identification of a novel antiandrogen with two bulky side chains, 6, which is a pure antagonist of the wild-type and the T877A, W741C, and H874Y mutated androgen receptors (AR), showing no cross-reactivity with progesterone receptor and low micromolar cytotoxicity in LNCaP, PCa-2b, 22Rv1, and C4-2B prostate cancer cells. Molecular modeling...
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