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  • Title: Design and synthesis of androgen receptor antagonists with bulky side chains for overcoming antiandrogen resistance.
    Author: Zhou J, Geng G, Shi Q, Sauriol F, Wu JH.
    Journal: J Med Chem; 2009 Sep 10; 52(17):5546-50. PubMed ID: 19725582.
    Abstract:
    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 indicates 6 adopts a "Y"-shape conformation and forms multiple hydrogen bonds with AR backbone.
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