Design of potent IGF1-R inhibitors related to bis-azaindoles.
Nemecek C., Metz W.A., Wentzler S., Ding F.X., Venot C., Souaille C., Dagallier A., Maignan S., Guilloteau J.P., Bernard F., Henry A., Grapinet S., Lesuisse D.
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.
Chem. Biol. Drug Des. 76:100-106(2010) [PubMed] [Europe PMC]