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Bioorg Med Chem Lett. 2009 Dec 1;19(23):6691-5. doi: 10.1016/j.bmcl.2009.09.123. Epub 2009 Oct 12.

Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.

Author information

1
Genomics Institute of the Novartis Research Foundation (GNF), San Diego, CA 92121, USA. gzhang@gnf.org

Abstract

A series of 4-amino-6-benzimidazole-pyrimidines was designed to target lymphocyte-specific tyrosine kinase (Lck), a member of the Src-family kinases (SFKs). These type II inhibitors were optimized using a cellular Lck-dependent proliferation assay and are capable of inhibiting Lck at single-digit nanomolar concentrations. This scaffold is likely to serve a valuable template for developing potent inhibitors of a number of SFKs.

PMID:
19854052
DOI:
10.1016/j.bmcl.2009.09.123
[Indexed for MEDLINE]

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