| Literature DB >> 16458511 |
Christine M Tarby1, 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.
Abstract
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 104 nM) with good anti-proliferative activity in A2780 cells (IC50 234 nM).Entities:
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Year: 2006 PMID： 16458511 DOI： 10.1016/j.bmcl.2006.01.056
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823