Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369983 | Bioorganic & Medicinal Chemistry Letters | 2012 | 7 Pages |
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
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Authors
Vadim Y. Dudkin, Cheng Wang, Kenneth L. Arrington, Mark E. Fraley, George D. Hartman, Steven M. Stirdivant, Robert A. Drakas, Keith Rickert, Eileen S. Walsh, Kelly Hamilton, Carolyn A. Buser, James Hardwick, Weikang Tao, Stephen C. Beck, Xianzhi Mao,