The discovery of a potent orally efficacious indole androgen receptor antagonist through in vivo screening

…, MT Lai, O Linton, DW Hahn, SG Lundeen, Z Sui

文献索引：Lanter, James C.; Fiordeliso, James J.; Jiang, Weiqin; Allan, George F.; Lai, Muh-Tsann; Linton, Olivia; Hahn, Do Won; Lundeen, Scott G.; Sui, Zhihua Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 1 p. 123 - 126

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被引用次数: 25

摘要

A series of novel 2-(1H-indol-2-yl)-propan-2-ols have been designed, synthesized, and screened for their ability to inhibit testosterone-induced prostate weight increases in immature rats. Through the use of this paradigm, we were able to identify compounds that exhibited in vivo potency equal to that of the marketed antiandrogen Casodex® when orally administered.