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

…, J Lao, A Gerken, T Tuntland, B Liu, J Chang…

Index: Alper, Phil B.; Marsilje, Thomas H.; Mutnick, Daniel; Lu, Wenshuo; Chatterjee, Arnab; Roberts, Michael J.; He, Yun; Karanewsky, Donald S.; Chow, Donald; Lao, Jianmin; Gerken, Andrea; Tuntland, Tove; Liu, Bo; Chang, Jonathan; Gordon, Perry; Martin Seidel; Tian, Shin-Shay Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 19 p. 5255 - 5258

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Citation Number: 22

Abstract

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