| Title | Design and synthesis of androgen receptor antagonists with bulky side chains for overcoming antiandrogen resistance. | | Author(s) | Zhou J, Geng G, Shi Q, Sauriol F, Wu JH | | Institution | Montreal Centre for Experimental Therapeutics in Cancer, Segal Cancer Center, McGill University, Montreal, Quebec, Canada. | | Source | J Med Chem 2009 Sep 10; 52(17):5546-50. | | 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. | | Language | eng | | Pub Type(s) | Journal Article
Research Support, Non-U.S. Gov't
| | PubMed ID | 19725582 |
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