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Copper salt-catalyzed formation of a novel series of triazole–spirodienone conjugates with potent anticancer activity

机译:铜盐催化形成具有有效抗癌活性的新系列三唑-螺二烯酮共轭物

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Copper salt-catalyzed oxidative amination resulted in the formation of a novel series of triazole–spirodienone conjugates, 4-triazolyl-1-oxa-4-azaspiro[4,5]deca-6,9-dien-3,8-diones and 4-triazolyl-1-oxa-4-azaspiro[4,5]deca-6,9-dien-8-ones. A single crystal of compound 1p among them was grown and analyzed by X-ray crystallography. These compounds were evaluated for their antiproliferative activities against MDA-MB-231, HeLa, A549 and MCF-7 cell lines. Most of them showed moderate to high anticancer potency in the four cancer cell lines. The discovery of the triazole–spirodienone conjugates as cytotoxic agents against cancer cells may open up a new field in which these novel small molecules could be further explored as promising anticancer agents.
机译:铜盐催化的氧化胺化作用形成了一系列新的三唑-螺二烯酮共轭物,即4-triazolyl-1-oxa-4-azaspiro [4,5] deca-6,9-dien-3,8-diones和4-三唑基-1-氧杂-4-氮杂螺[4,5]癸-6,9-dien-8-ones。使其中的化合物1p的单晶生长并通过X射线晶体学分析。评价这些化合物对MDA-MB-231,HeLa,A549和MCF-7细胞系的抗增殖活性。他们中的大多数在四种癌细胞系中显示出中等至高的抗癌能力。三唑-螺二烯酮共轭物作为抗癌细胞毒性药物的发现可能会开辟一个新领域,在这些领域中,这些新的小分子可以作为有希望的抗癌剂进行进一步探索。

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