Discovery of 4-azaindoles as novel inhibitors of c-Met kinase

…, JM Gascon-Simorte, M Calmiano, K Le Riche…

Index: Porter, John; Lumb, Simon; Franklin, Richard J.; Gascon-Simorte, Jose M.; Calmiano, Mark; Riche, Kelly Le; Lallemand, Benedicte; Keyaerts, Jean; Edwards, Helen; Maloney, Alison; Delgado, Jean; King, Lloyd; Foley, Anne; Lecomte, Fabien; Reuberson, James; Meier, Christoph; Batchelor, Mark Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 10 p. 2780 - 2784

Full Text: HTML

Citation Number: 35

Abstract

A series of 4-azaindole inhibitors of c-Met kinase is described. The postulated binding mode was confirmed by an X-ray crystal structure and series optimisation was performed on the basis of this structure. Future directions for series development are discussed. ... The SAR and X-ray crystal structure of a series of 4-azaindole inhibitors of c-Met kinase is reported. ... Members of the receptor tyrosine kinase (RTK) family are attractive targets for cancer therapy as ...