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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, kinase inhibitory potencies and in vitro antiproliferative activity of isoindigo and 7'-azaisoindigo derivatives substituted by Sonogashira cross-coupling.
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Synthesis, kinase inhibitory potencies and in vitro antiproliferative activity of isoindigo and 7'-azaisoindigo derivatives substituted by Sonogashira cross-coupling.

机译：Sonogashira交叉偶联取代的异靛蓝和7'-氮杂异靛蓝衍生物的合成，激酶抑制效能和体外抗增殖活性。

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摘要

In the course of structure-activity relationship studies we were interested in the synthesis of isoindigo and 7'-azaisoindigo derivatives substituted at the N-1 position by a 1-(2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyl), at the 5'-position by various chains introduced by Sonogashira cross-coupling and substituted or not at the 5-position by a bromine atom. To get an insight into the substitution pattern required for the best biological potencies, their kinase inhibitory potencies and their in vitro antiproliferative activities were evaluated. The derivatives were tested toward four protein kinases (CDK5/p25, GSK3, CK1, Dyrk1A) and their in vitro antiproliferative activity was tested against two human myeloid leukaemia cell lines (K562 and HL60).
机译：在结构-活性关系研究过程中，我们对异靛蓝和7'-氮杂异靛蓝衍生物的合成感兴趣，这些衍生物在N-1位被1-（2,3,4,6-tetra-O-乙酰-β取代-D-吡喃葡萄糖基），在5'-位由Sonogashira交叉偶联引入的各种链，在5-位被溴原子取代或没有被溴原子取代。为了深入了解最佳生物学效能所需的替代模式，对它们的激酶抑制效能和体外抗增殖活性进行了评估。对该衍生物针对四种蛋白激酶（CDK5 / p25，GSK3，CK1，Dyrk1A）进行了测试，并针对两种人类骨髓白血病细胞系（K562和HL60）测试了其体外抗增殖活性。

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