Design of potent IGF1-R inhibitors related to bis-azaindoles.
Article Details
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Nemecek C, Metz WA, Wentzler S, Ding FX, Venot C, Souaille C, Dagallier A, Maignan S, Guilloteau JP, Bernard F, Henry A, Grapinet S, Lesuisse D
Design of potent IGF1-R inhibitors related to bis-azaindoles.
Chem Biol Drug Des. 2010 Aug;76(2):100-6. doi: 10.1111/j.1747-0285.2010.00991.x. Epub 2010 Jun 9.
- PubMed ID
- 20545947 [ View in PubMed]
- Abstract
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.