Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP

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• 作者：Anthony J. Roecker ; Paul J. Coleman ; Swati P. Mercer ; John D. Schreier ; Carolyn A. Buser ; Eileen S. Walsh ; Kelly Hamilton ; Robert B. Lobell ; Weikang Tao ; Ronald E. Diehl ; Vicki J. South ; Joseph P. Dav
• 关键词：KSP inhibitors ; Antimitotics ; Pgp ; Kinesins ; 1 ; 4-Diaryl-4 ; 5-dihydropyrazoles ; Copper-mediated N-arylation ; Kinesin spindle protein ; Cancer
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 October 2007
• 卷：17
• 期：20
• 页码：5677-5682
• 文件大小：241 K

摘要

Inspired by previous efforts in the pyrazolobenzoxazine class of KSP inhibitors, the design and synthesis of 1,4-diaryl-4,5-dihydropyrazole inhibitors of KSP are described. Crystallographic evidence of binding mode and in vivo potency data is also highlighted.