2. Academic Validation
  3. Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: advantages in comparison with competitive inhibitors

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

Affiliation

  • 1 Medicinal Chemistry, Sanofi-aventis, 13 Quai Jules Guesde, 94300 Vitry-sur-Seine, France. dominique.lesuisse@sanofi-aventis.com
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.

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