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

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• 作者：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
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：June 9, 2016
• 年：2016
• 卷：7
• 期：6
• 页码：595-600
• 全文大小：414K
• 年卷期：0
• ISSN：1948-5875

文摘

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.