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Bioorg Med Chem Lett. 2010 Dec 15;20(24):7216-21. doi: 10.1016/j.bmcl.2010.10.105. Epub 2010 Oct 26.

Design, synthesis and SAR of thienopyridines as potent CHK1 inhibitors.

Author information

1
Department of Chemistry, Merck Research Laboratories, Cambridge, MA 02141, USA. lianyun.zhao@merck.com

Abstract

A novel series of CHK1 inhibitors based on thienopyridine template has been designed and synthesized. These inhibitors maintain critical hydrogen bonding with the hinge and conserved water in the ATP binding site. Several compounds show single digit nanomolar CHK1 activities. Compound 70 shows excellent enzymatic activity of 1 nM.

PMID:
21074424
DOI:
10.1016/j.bmcl.2010.10.105
[Indexed for MEDLINE]

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