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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and cytotoxic activity of 2-methylimidazo(1,2-a)pyridine- and quinoline-substituted 2-aminopyrimidine derivatives.
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Synthesis and cytotoxic activity of 2-methylimidazo(1,2-a)pyridine- and quinoline-substituted 2-aminopyrimidine derivatives.

机译：2-甲基咪唑并（1,2-a）吡啶和喹啉取代的2-氨基嘧啶衍生物的合成及细胞毒活性。

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摘要

A series of 2-methylimidazo[1,2-a]pyridine- and quinoline-substituted 2-aminopyrimidines derivatives were synthesized using a convenient synthetic route. We evaluate the isosteric replacement of methyl groups in 4-(2-methylimidazo[1,2-a]pyridin-3-yl)-N-p-tolylpyrimidin-2-amine (compound 1) by trifluoromethyl groups and the isosteric substitution of the 2-methylimidazo[1,2-a]pyridin-3-yl scaffold by quinolin-4-yl or quinolin-3-yl moieties. The replacement of hydrogen by fluorine does not affect notably the cytotoxic activity and CDK inhibitor activity in this series. Quinolin-4-yl-substituted compound, 8, presents cytotoxic activity and is most effective and selective against CDK1/CycA than against CDK2/CycB. Compound 11, which has a quinolin-3-yl moiety is CDK inhibitor but presents null cytotoxic activity. Quinolin-4-yl-substituted compounds constitute a new lead of cytotoxic and CDK inhibitor compounds from which more compelling and selective inhibitors can be designed.
机译：使用方便的合成途径合成了一系列2-甲基咪唑并[1,2-a]吡啶-和喹啉取代的2-氨基嘧啶衍生物。我们评估三氟甲基基团的4-（2-甲基咪唑并[1,2-a]吡啶-3-基）-Np-甲苯基嘧啶-2-胺（化合物1）中甲基的等位取代及2的等位取代-甲基咪唑并[1,2-a]吡啶-3-基骨架由喹啉-4-基或喹啉-3-基部分组成。用氟代替氢不会显着影响该系列中的细胞毒活性和CDK抑制剂活性。喹啉-4-基取代的化合物8具有细胞毒性，对CDK1 / CycA的作用最强，对CDK2 / CycB的作用最强。具有喹啉-3-基部分的化合物11是CDK抑制剂，但没有细胞毒活性。喹啉-4-基取代的化合物构成了细胞毒性和CDK抑制剂化合物的新先导，从中可以设计出更具吸引力和选择性的抑制剂。

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