The discovery of a potent orally efficacious indole androgen receptor antagonist through in vivo screening
作者:James C. Lanter、James J. Fiordeliso、Weiqin Jiang、George F. Allan、Muh-Tsann Lai、Olivia Linton、Do Won Hahn、Scott G. Lundeen、Zhihua Sui
DOI:10.1016/j.bmcl.2006.09.086
日期:2007.1
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 (R) when orally administered. (c) 2006 Elsevier Ltd. All rights reserved.