Discovery and biological evaluation of benzo[a] carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor

被引：26

作者：

Alper, Phil B. ^{[1
]}

Marsilje, Thomas H. ^{[1
]}

Mutnick, Daniel ^{[1
]}

Lu, Wenshuo ^{[1
]}

Chatterjee, Arnab ^{[1
]}

Roberts, Michael J. ^{[1
]}

He, Yun ^{[1
]}

Karanewsky, Donald S. ^{[1
]}

Chow, Donald ^{[1
]}

Lao, Jianmin ^{[1
]}

Gerken, Andrea ^{[1
]}

Tuntland, Tove ^{[1
]}

Liu, Bo ^{[1
]}

Chang, Jonathan ^{[1
]}

Gordon, Perry ^{[1
]}

Seidel, H. Martin ^{[1
]}

Tian, Shin-Shay ^{[1
]}

机构：

[1] Novartis Res Fdn GNF, Genom Inst, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 19期

关键词：

Tpo; thrombopoietin; TpoR; cMpl; hematopoietic growth factor; agonist;

D O I：

10.1016/j.bmcl.2008.08.068

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of benzo[a] carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor is reported. Starting from a 3.4 mu M high throughput screen hit, members of this series have been identified which are full agonists with functional potency < 50 nM and oral bioavailability in mice. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：5255 / 5258

页数：4

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