Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer
Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer
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DOI：
10.1016/j.bmcl.2011.01.071
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发表时间：
2011-03-01
影响因子：
2.7
通讯作者：
Zhou, Feng
中科院分区：
文献类型：
--
作者：
Dong, Qing;Dougan, Douglas R.;Zhou, Feng
采用基于结构的药物设计方法，开发了一种新的5-苯氨基-8-甲基吡啶并[2，3-d]嘧啶-4，7（3 H，8H）-二酮系列MEK抑制剂。该系列的先导化合物优化导致TAK-733的发现。该研究已进入癌症治疗的I期临床研究。(C)2011爱思唯尔有限公司版权所有。
A novel 5-phenylamino-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione series of MEK inhibitors has been developed using structure-based drug design. Lead optimization of this series led to the discovery of TAK-733. This was advanced to Phase I clinical studies for cancer treatment. (C) 2011 Elsevier Ltd. All rights reserved.