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Proline isosteres in a series of 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitors of IGF-1R kinase and IR kinase.

Sampognaro, Anthony J; Wittman, Mark D; Carboni, Joan M; Chang, Chiehying; Greer, Ann F; Hurlburt, Warren W; Sack, John S; Vyas, Dolatrai M.
Bioorg Med Chem Lett; 20(17): 5027-30, 2010 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-20675137
Pyrrolidine, pyrrolidinone, carbocyclic, and acyclic groups were used as isosteric proline replacements in a series of insulin-like growth factor I receptor kinase/insulin receptor kinase inhibitors. Examples that were similar in potency to proline-containing reference compounds were shown to project a key fluoropyridine amide into a common space, while less potent compounds were not able to do so for reasons of stereochemistry or structural rigidity.
Selo DaSilva