866319-39-3Relevant articles and documents
Design of potent IGF1-R inhibitors related to bis-azaindoles
Nemecek, Conception,Metz, William A.,Wentzler, Sylvie,Ding, Fa-Xiang,Venot, Corinne,Souaille, Catherine,Dagallier, Anne,Maignan, Sebastien,Guilloteau, Jean-Pierre,Bernard, Francois,Henry, Alain,Grapinet, Sandrine,Lesuisse, Dominique
, p. 100 - 106 (2011/03/19)
From an azaindole lead, identified in high throughput screen, a series of potent bis-azaindole inhibitors of IGF1-R have been synthesized using rational drug design and SAR based on a in silico binding mode hypothesis. Although the resulting compounds produced the expected improved potency, the model was not validated by the co-crystallization experiments with IGF1-R.
