Discovery of thiophene inhibitors of polo-like kinase

被引:38
作者
Emmitte, Kyle A. [1 ]
Andrews, C. Webb [1 ]
Badiang, Jennifer G. [1 ]
Davis-Ward, Ronda G. [1 ]
Dickson, Hamilton D. [1 ]
Drewry, David H. [1 ]
Emerson, Holly K. [1 ]
Epperly, Andrea H. [1 ]
Hassler, Daniel F. [1 ]
Knick, Victoria B. [1 ]
Kuntz, Kevin W. [1 ]
Lansing, Timothy J. [1 ]
Linn, James A. [1 ]
Mook, Robert A., Jr. [1 ]
Nailor, Kristen E. [1 ]
Salovich, James M. [1 ]
Spehar, Glenn M. [1 ]
Cheung, Mui [1 ]
机构
[1] GlaxoSmithKline, Oncol R & D, Res Triangle Pk, NC 27709 USA
关键词
Thiophene; Benzimidazole; Polo-like kinase; Mitosis; Inhibitor; Cell-cycle; PLK1;
D O I
10.1016/j.bmcl.2008.11.041
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The discovery and development of a series of thiophenes as potent and selective inhibitors of PLK is described. Identification and characterization of 2, a useful in vitro PLK inhibitor tool compound, is also presented. (C) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1018 / 1021
页数:4
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