Article
Antiandrogenic, maspin induction, and antiprostate cancer activities of tanshinone IIA and its novel derivatives with modification in ring A.
Journal of medicinal chemistry - 26 Jan 2012
Liu Weiguo, Zhou Jinming, Geng Guoyan, Shi Qingwen, Sauriol Francoise, Wu Jian Hui
Abstract excerpt
Expression of metastatic suppressor maspin is lost in advanced prostate cancer. Clinically relevant mutations in androgen receptor (AR) convert antiandrogens into AR agonists, promoting prostate tumor growth. We discovered tanshinone IIA (TS-IIA) is a potent antagonist of mutated ARs and induces maspin expression through AR. TS-IIA suppressed AR expression and induced apoptosis in LNCaP cells. Syntheses of TS-IIA...
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