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

Philippe Bergeron,Michael F T Koehler,Elizabeth M Blackwood,Krista Bowman,Kevin Clark,Ron Firestein,James R Kiefer,Klaus Maskos,Mark L McCleland,Linda Orren, Sreemathy Ramaswamy,Laurent Salphati,Steve Schmidt, Elisabeth V Schneider,Jiansheng Wu,Maureen Beresini

ACS medicinal chemistry letters（2016）

Cited 45|Views46

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Abstract

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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