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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.

Bioorganic & medicinal chemistry letters 2010 Jul 15; In press

Link to PubMed abstract

Sampognaro A AJ, Wittman M MD, Carboni J JM, Chang C, Greer A AF, Hurlburt W WW, Sack J JS, Vyas D DM

Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, P.O. Box 5400, Princeton, NJ 08543-5400, USA.

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.

Keywords: IGF-1R kinase