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Bioorg Med Chem Lett. 2007 Jan 1;17(1):123-6. Epub 2006 Sep 30.

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

Author information

1
Johnson & Johnson Pharmaceutical Research and Development L.L.C., 666 Stockton Drive, Exton, PA 19341, USA. jlanter@prdus.jnj.com

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.

PMID:
17071085
DOI:
10.1016/j.bmcl.2006.09.086
[Indexed for MEDLINE]
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