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Design of Potent IGF1‐R Inhibitors Related to Bis‐azaindoles
Author(s) -
Nemecek Conception,
Metz William A.,
Wentzler Sylvie,
Ding FaXiang,
Venot Corinne,
Souaille Catherine,
Dagallier Anne,
Maignan Sébastien,
Guilloteau JeanPierre,
Bernard François,
Henry Alain,
Grapinet Sandrine,
Lesuisse Dominique
Publication year - 2010
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2010.00991.x
Subject(s) - in silico , potency , rational design , chemistry , combinatorial chemistry , drug design , computational biology , stereochemistry , drug , drug discovery , pharmacology , in vitro , biochemistry , biology , genetics , gene
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.