title: Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: advantages in comparison with competitive inhibitors.
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.
authors: Medicinal Chemistry, Sanofi-aventis, 13 Quai Jules Guesde, 94300 Vitry-sur-Seine, France. dominique.lesuisse@sanofi-aventis.com
authors: Dominique
authors: D
authors: Lesuisse
authors: Jacques
authors: J
authors: Mauger
authors: Conception
authors: C
authors: Nemecek
authors: Sébastien
authors: S
authors: Maignan
authors: Janine
authors: J
authors: Boiziau
authors: Greg
authors: G
authors: Harlow
authors: Augustin
authors: A
authors: Hittinger
authors: Swen
authors: S
authors: Ruf
authors: Hartmut
authors: H
authors: Strobel
authors: Anil
authors: A
authors: Nair
authors: Kurt
authors: K
authors: Ritter
authors: Jean-Luc
authors: JL
authors: Malleron
authors: Anne
authors: A
authors: Dagallier
authors: Youssef
authors: Y
authors: El-Ahmad
authors: Jean-Pierre
authors: JP
authors: Guilloteau
authors: Houlfa
authors: H
authors: Guizani
authors: Hervé
authors: H
authors: Bouchard
authors: Corinne
authors: C
authors: Venot
mesh_terms: D000255:Adenosine Triphosphate / Q000737:chemistry; D000818:Animals; D001665:Binding Sites; D001667:Binding, Competitive; D003198:Computer Simulation; D004353:Drug Evaluation, Preclinical; D051379:Mice; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D017526:Receptor, IGF Type 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D047428:Protein Kinase Inhibitors; D000255:Adenosine Triphosphate; D017526:Receptor, IGF Type 1