Akue-Gedu Rufine, Debiton Eric, Ferandin Yoan, Meijer Laurent, Prudhomme Michelle, Anizon Fabrice, Moreau Pascale
Clermont Université, Université Blaise Pascal, SEESIB, Aubière, France.
Bioorg Med Chem. 2009 Jul 1;17(13):4420-4. doi: 10.1016/j.bmc.2009.05.017. Epub 2009 May 12.
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, CK1delta/epsilon, GSK-3alpha/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).
描述了在2-氨基嘧啶环的C-5位被各种芳基取代且吲哚氮上有或没有甲基取代的新meridianin衍生物的合成。测试了这些化合物对五种激酶（CDK5/p25、CK1δ/ε、GSK-3α/β、Dyrk1A和Erk2）的激酶抑制活性，以及它们对人原代成纤维细胞培养物和两种人实体癌细胞系（MCF-7和PA 1）的体外抗增殖活性。
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