2. Academic Validation
  3. Discovery of non-LBD inhibitor for androgen receptor by structure-guide design

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

Affiliation

  • 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.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z