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Bioorg Med Chem Lett. 2012 Apr 1;22(7):2613-9. doi: 10.1016/j.bmcl.2012.01.120. Epub 2012 Feb 7.

Pyridyl aminothiazoles as potent Chk1 inhibitors: optimization of cellular activity.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. vadim_dudkin@merck.com

Abstract

Translation of significant biochemical activity of pyridyl aminothiazole class of Chk1 inhibitors into functional CEA potency required analysis and adjustment of both physical properties and kinase selectivity profile of the series. The steps toward optimization of cellular potency included elimination of CDK7 activity, reduction of molecular weight and polar surface area and increase in lipophilicity of the molecules in the series.

PMID:
22365762
DOI:
10.1016/j.bmcl.2012.01.120
[Indexed for MEDLINE]

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