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Bioorg Med Chem Lett. 2003 Nov 17;13(22):4007-10.

Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).

Author information

1
Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. jwityak@gnf.org

Abstract

A novel series of 2-amino-5-carboxamidothiazoles were identified as inhibitors of Lck. Structure-activity studies demonstrate the structural requirements for potent Lck activity. Cyclopropylamide 11d is a potent Lck inhibitor having sub-micromolar activity in a PBL proliferation assay.

PMID:
14592495
DOI:
10.1016/j.bmcl.2003.08.054
[Indexed for MEDLINE]

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