Synthesis and biological activities of aminopyrimidyl-indoles structurally related to meridianins
Synthesis and biological activities of aminopyrimidyl-indoles structurally related to meridianins
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DOI：
10.1016/j.bmc.2009.05.017
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发表时间：
2009-07-01
影响因子：
3.5
通讯作者：
Moreau, Pascale
中科院分区：
文献类型：
--
作者：
Akue-Gedu, Rufine;Debiton, Eric;Moreau, Pascale
报道了在2-氨基嘧啶环的C-5位被各种芳基取代或不被吲哚氮上的甲基取代的新的子午素衍生物的合成。测试了这些化合物对5种激酶(CDK5/p25、CK1 Delta/epsilon、GSK-3α/β、Dyrk1A和ERK2)的抑制活性，以及它们对人成纤维细胞原代培养和两种人实体癌细胞株(MCF-7和PA 1)的体外抗增殖活性。(C)2009爱思唯尔有限公司。保留所有权利。
The synthesis of new meridianin derivatives substituted at the C-5 position of the 2-aminopyrimidine ring by various aryl groups and substituted or not by a methyl group on the indole nitrogen is described. These compounds were tested for their kinase inhibitory potencies toward five kinases (CDK5/p25, CK1 delta/epsilon, GSK-3 alpha/beta, Dyrk1A and Erk2) as well as their in vitro antiproliferative activities toward a human fibroblast primary culture and two human solid cancer cell lines (MCF-7 and PA 1). (C) 2009 Elsevier Ltd. All rights reserved.