Design of Potent IGF1‐R Inhibitors Related to Bis‐azaindoles
Copyright policy )Design of Potent IGF1‐R Inhibitors Related to Bis‐azaindoles
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.
- Sanofi (France) France
Binding Sites, Indoles, Crystallography, X-Ray, Mice, Structure-Activity Relationship, Cell Line, Tumor, Drug Design, Animals, Humans, Drug Screening Assays, Antitumor, Insulin-Like Growth Factor I, Protein Kinase Inhibitors
Binding Sites, Indoles, Crystallography, X-Ray, Mice, Structure-Activity Relationship, Cell Line, Tumor, Drug Design, Animals, Humans, Drug Screening Assays, Antitumor, Insulin-Like Growth Factor I, Protein Kinase Inhibitors
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