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

  • Bioorg Med Chem Lett. 2013 Jul 1;23(13):3887-90. doi: 10.1016/j.bmcl.2013.04.065.
Byung Jun Ryu  1 ,  Nakjeong Kim ,  Jun Tae Kim ,  Tae-Sung Koo ,  Sung-Eun Yoo ,  Seo Hee Jeong ,  Seong Hwan Kim ,  Nam Sook Kang
Affiliations
  • 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.
PMID: 23727044 DOI: 10.1016/j.bmcl.2013.04.065
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.