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

  • Bioorg Med Chem Lett. 2008 Oct 1;18(19):5255-8. doi: 10.1016/j.bmcl.2008.08.068.
Phil B Alper  1 ,  Thomas H Marsilje ,  Daniel Mutnick ,  Wenshuo Lu ,  Arnab Chatterjee ,  Michael J Roberts ,  Yun He ,  Donald S Karanewsky ,  Donald Chow ,  Jianmin Lao ,  Andrea Gerken ,  Tove Tuntland ,  Bo Liu ,  Jonathan Chang ,  Perry Gordon ,  H Martin Seidel ,  Shin-Shay Tian
Affiliations
  • 1. Genomics Institute of the Novartis Research Foundation (GNF), San Diego, CA 92121, USA.
PMID: 18778936 DOI: 10.1016/j.bmcl.2008.08.068
Abstract

A novel series of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor is reported. Starting from a 3.4 microM 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.

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