Inhibitors of human mitotic kinesin Eg5: Characterization of the 4-phenyl-tetrahydroisoquinoline lead series

Christine M. Tarby,Robert F. Kaltenbach,Tram Huynh,Andrew Pudzianowski,Henry Shen,Marie Ortega-Nanos,Steven Sheriff,John A. Newitt,Patricia A. McDonnell,Neil Burford,Craig R. Fairchild,Wayne Vaccaro,Zhong Chen,Robert M. Borzilleri,Joseph Naglich,Louis J. Lombardo,Marco Gottardis,George L. Trainor,Deborah L. Roussell

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

In a high-throughput screening effort, a series of tetrahydroisoquinolines was identified as modest inhibitors of human Eg5. A medicinal chemistry optimization effort led to the identification of R-4-(3-hydroxyphenyl)-N,N-7,8-tetramethyl-3,4-dihydroisoquinoline-2(1H)-carboxamide (32a) as a potent inhibitor of human Eg5 (ATPase IC50 104nM) with good anti-proliferative activity in A2780 cells (IC50 234nM).

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关键词

Eg5 inhibitor,Kinesin inhibitor,Kinesin spindle protein,KSP,Eg5

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