4.5 Article

Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8

Journal

ACS MEDICINAL CHEMISTRY LETTERS
Volume 7, Issue 6, Pages 595-600

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.6b00044

Keywords

Sorafenib; CDK8; inhibitor; DMG-out

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Using Sorafenib as a starting point, a series of potent and selective inhibitors of CDK8 was developed. When cocrystallized with CDK8 and cyclin C, these compounds exhibit a Type-II (DMG-out) binding mode.

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