The discovery of a potent orally efficacious indole androgen receptor antagonist through in vivo screening |
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| Authors: | Lanter James C Fiordeliso James J Jiang Weiqin Allan George F Lai Muh-Tsann Linton Olivia Hahn Do Won Lundeen Scott G Sui Zhihua |
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| Affiliation: | Johnson & Johnson Pharmaceutical Research and Development L.L.C., 666 Stockton Drive, Exton, PA 19341, USA. jlanter@prdus.jnj.com |
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| Abstract: | ![]()
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. |
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