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Bioorg Med Chem Lett. 2010 Sep 1;20(17):5027-30. doi: 10.1016/j.bmcl.2010.07.045. Epub 2010 Jul 15.

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.

Author information

1
Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, USA. anthony.sampognaro@bms.com

Abstract

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.

PMID:
20675137
DOI:
10.1016/j.bmcl.2010.07.045
[Indexed for MEDLINE]

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