Article ID Journal Published Year Pages File Type
1369983 Bioorganic & Medicinal Chemistry Letters 2012 7 Pages PDF
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.

Graphical abstractThe optimization of selectivity and physical properties of pyridyl aminothiazole series of Chk1 inhibitors aimed at improving cellular activity levels is described.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
Authors
, , , , , , , , , , , , , , ,