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Synthesis and in Vitro Antiproliferative Activity of New Phenylaminoisoquinolinequinones against Cancer Cell Lines

机译:新型苯氨基异喹啉喹啉酮类化合物的合成及其体外抗增殖活性

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摘要

A variety of phenylaminoisoquinolinequinones were synthesized and tested for their antiproliferative activity against three human-tumor derived cancer cell lines. The new aminoquinones were prepared from 4-methoxycarbonyl-3-methylisoquinoline-5,8- quinone (1) via acid-induced amination and bromination reactions. Remarkable differences in antiproliferative activity were observed depending upon the location and donor capacity of the substituted phenylamino group at the quinone nucleus. The effect of the substituents on the biological activity is discussed in terms of the donor-acceptor interactions which were evaluated through the redox properties of the aminoquinones.
机译:合成了多种苯基氨基异喹啉醌,并测试了它们对三种人类肿瘤来源的癌细胞系的抗增殖活性。新的氨基醌是由4-甲氧基羰基-3-甲基异喹啉-5,8-醌(1)经酸诱导的胺化和溴化反应制得的。观察到抗增殖活性的显着差异,这取决于取代的苯氨基在醌核上的位置和供体能力。通过供体-受体相互作用讨论了取代基对生物活性的影响,其通过氨基醌的氧化还原性质进行了评估。

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