917231-35-7Relevant academic research and scientific papers
Pyridyl aminothiazoles as potent Chk1 inhibitors: Optimization of cellular activity
Dudkin, Vadim Y.,Wang, Cheng,Arrington, Kenneth L.,Fraley, Mark E.,Hartman, George D.,Stirdivant, Steven M.,Drakas, Robert A.,Rickert, Keith,Walsh, Eileen S.,Hamilton, Kelly,Buser, Carolyn A.,Hardwick, James,Tao, Weikang,Beck, Stephen C.,Mao, Xianzhi,Lobell, Robert B.,Sepp-Lorenzino, Laura
, p. 2613 - 2619 (2012/05/05)
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.
INHIBITORS OF CHECKPOINT KINASES
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Page/Page column 98; 100, (2008/06/13)
The instant invention provides for compounds which comprise substituted pyridyl aminothiazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.
