Antiandrogenic, Maspin Induction, and Antiprostate Cancer Activities of Tanshinone IIA and Its Novel Derivatives with Modification in Ring A

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• 作者：Weiguo Liu ; Jinming Zhou ; Guoyan Geng ; Qingwen Shi ; Francoise Sauriol ; Jian Hui Wu
• 刊名：Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：January 26, 2012
• 年：2012
• 卷：55
• 期：2
• 页码：971-975
• 全文大小：294K
• 年卷期：v.55,no.2(January 26, 2012)
• ISSN：1520-4804

文摘

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 derivatives (1鈥?b>9) revealed that the 4,4-dimethyl group at ring A is important for TS-IIA鈥檚 antiandrogenic and maspin induction activities.