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Bioorg Med Chem Lett. 2013 Jul 1;23(13):3887-90. doi: 10.1016/j.bmcl.2013.04.065. Epub 2013 May 3.

Discovery of non-LBD inhibitor for androgen receptor by structure-guide design.

Author information

1
Laboratory of Translational Therapeutics, Pharmacology Research Center, Division of Drug Discovery Research, Korea Research Institute of Chemical Technology, P.O. Box 107, Yuseong-gu, Daejeon 305-600, Republic of Korea.

Abstract

In this study, we synthesized the BF-3 binding small molecules, a series of pyridazinone-based compounds, as a novel class of non-LBP antiandrogens for treating prostate cancer by inhibiting androgen receptor. The new class compound was discovered to inhibitor the viability of AR-dependent human prostate LNCap cells and AR activity combining with the computational method. It showed a good physicochemical and PK property.

PMID:
23727044
DOI:
10.1016/j.bmcl.2013.04.065
[Indexed for MEDLINE]

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