Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor
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.
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.