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Synthesis, Cytotoxicity and Topoisomerase II Inhibition Study of New Thioxanthone Analogues

机译:新型噻吨酮类似物的合成,细胞毒性和拓扑异构酶II抑制研究

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摘要

Xanthone (1) compounds found as secondary metabolites from higher plants and microorganisms have wide biological profiles including anti-hypertensive, anti-oxidative, antithrombotic, and anti-cancer activity, based on their diverse structures. The interesting structural scaffold and biological efficacy of xanthones enforced many scientists to synthesize these compounds for the development of prospective new drug candidates. Among these xanthones, oxygenated xanthones synthesized or isolated from natural sources revealed effective inhibitory activity against several cancer cell lines. Especially, 2',3'-epoxypropoxy substituted xanthones have efficiently prohibited growth of cancer cells and xanthone (2) possessing two 2',3'-epoxypropoxy groups at 3 and 5 position showed most active anticancer activity in the series prepared.
机译:黄嘌呤(1)化合物是高等植物和微生物的次生代谢产物,其结构多样,具有广泛的生物学特性,包括抗高血压,抗氧化,抗血栓形成和抗癌活性。氧杂蒽的有趣的结构支架和生物学功效迫使许多科学家合成这些化合物以开发预期的新药候选物。在这些氧杂蒽酮中,从天然来源合成或分离的含氧氧杂蒽酮显示出对几种癌细胞系的有效抑制活性。特别是,2',3'-环氧丙氧基取代的x吨酮有效地抑制了癌细胞的生长,在制备的系列中,在3和5位具有两个2',3'-环氧丙氧基的蒽酮(2)具有最强的抗癌活性。

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