Design of Potent IGF1-R Inhibitors Related to Bis-azaindoles


Corresponding author: Dominique Lesuisse,


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.