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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, biological evaluation, and molecular docking study of 3-(3'-heteroatom substituted-2'-hydroxy-1'-propyloxy) xanthone analogues as novel topoisomerase IIalpha catalytic inhibitor.
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Synthesis, biological evaluation, and molecular docking study of 3-(3'-heteroatom substituted-2'-hydroxy-1'-propyloxy) xanthone analogues as novel topoisomerase IIalpha catalytic inhibitor.

机译：作为新型拓扑异构酶IIα催化抑制剂的3-（3'-杂原子取代的2'-羟基-1'-丙氧基）蒽酮类似物的合成，生物学评估和分子对接研究。

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摘要

Epoxide ring-opened xanthone derivatives were synthesized and tested for their topoisomerase inhibitory activity and cytotoxicity. Most of the compounds showed topo IIalpha specific inhibitory activity. To clarify the mechanism of action of these compounds, the most potent compound (compound 14) of the synthesized analogues was further studied by testing its ATPase inhibitory activity and through molecular docking experiments. The results showed that the topo IIalpha inhibitory activity of compound 14 was inversely proportional to ATP concentration. In the ATPase inhibitory test, ATP hydrolysis was reduced less efficiently by compound 14 (28.5+/-4.6%) than novobiocin (60.4+/-8.1%). Molecular docking study revealed compound 14 to have a stable binding pattern to the ATP-binding domain of human topo II.
机译：合成了环氧化物开环的x吨酮衍生物，并测试了它们的拓扑异构酶抑制活性和细胞毒性。大多数化合物表现出topo IIalpha特异性抑制活性。为了阐明这些化合物的作用机理，通过测试其ATPase抑制活性并通过分子对接实验进一步研究了合成类似物中最有效的化合物（化合物14）。结果表明，化合物14的topo IIalpha抑制活性与ATP浓度成反比。在ATPase抑制试验中，化合物14（28.5 +/- 4.6％）的还原效率比新霉素（60.4 +/- 8.1％）降低的效率更低。分子对接研究表明化合物14与人topo II的ATP结合域具有稳定的结合模式。

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