Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: advantages in comparison with competitive inhibitors

  • Bioorg Med Chem Lett. 2011 Apr 15;21(8):2224-8. doi: 10.1016/j.bmcl.2011.03.003.
Dominique Lesuisse  1 ,  Jacques Mauger ,  Conception Nemecek ,  Sébastien Maignan ,  Janine Boiziau ,  Greg Harlow ,  Augustin Hittinger ,  Swen Ruf ,  Hartmut Strobel ,  Anil Nair ,  Kurt Ritter ,  Jean-Luc Malleron ,  Anne Dagallier ,  Youssef El-Ahmad ,  Jean-Pierre Guilloteau ,  Houlfa Guizani ,  Hervé Bouchard ,  Corinne Venot
Affiliations
  • 1. Medicinal Chemistry, Sanofi-aventis, 13 Quai Jules Guesde, 94300 Vitry-sur-Seine, France. [email protected]
PMID: 21441024 DOI: 10.1016/j.bmcl.2011.03.003
Abstract

A new series of IGF-1R inhibitors related to hydantoins were identified from a lead originating from HTS. Their noncompetitive property as well as their slow binding characteristics provided a series of compounds with unique selectivity and excellent cellular activities.