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

Authors :
Elizabeth Blackwood
Linda Orren
Klaus Maskos
Mark McCleland
Sreemathy Ramaswamy
Laurent Salphati
Jiansheng Wu
James R. Kiefer
Maureen Beresini
Ron Firestein
Steve Schmidt
E.V. Schneider
Philippe Bergeron
Krista K. Bowman
Michael F. T. Koehler
Kevin R Clark
Source :
ACS medicinal chemistry letters. 7(6)
Publication Year :
2016

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.

Details

ISSN :
19485875
Volume :
7
Issue :
6
Database :
OpenAIRE
Journal :
ACS medicinal chemistry letters
Accession number :
edsair.doi.dedup.....8dbe04b31fbb281e1028cfa39678c3de