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铜盐催化形成具有强效抗癌活性的新型三唑-螺二烯酮共轭物系列。

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

作者信息

Gu Linghui, Wang Peng, Zhong Qiu, Deng Yuxing, Xie Jiangping, Liu Fei, Xiao Fan, Zheng Shilong, Chen Yue, Wang Guangdi, He Ling

机构信息

Key Laboratory of Drug-Targeting and Drug-Delivery Systems of the Ministry of Education, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu, 610041, China.

RCMI Cancer Research Center, Xavier University of Louisiana, New Orleans, LA 70125, USA.

出版信息

RSC Adv. 2017;7(16):9412-9416. doi: 10.1039/C6RA24764D. Epub 2017 Jan 30.

Abstract

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 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.

摘要

铜盐催化的氧化胺化反应生成了一系列新型的三唑-螺二烯酮共轭物,即4-三唑基-1-氧杂-4-氮杂螺[4,5]癸-6,9-二烯-3,8-二酮和4-三唑基-1-氧杂-4-氮杂螺[4,5]癸-6,9-二烯-8-酮。其中一种化合物的单晶被培养出来并通过X射线晶体学进行分析。对这些化合物针对MDA-MB-231、HeLa、A549和MCF-7细胞系的抗增殖活性进行了评估。它们中的大多数在这四种癌细胞系中显示出中等至高的抗癌效力。作为抗癌细胞的细胞毒性剂的三唑-螺二烯酮共轭物的发现可能会开辟一个新领域,在这个领域中这些新型小分子可以作为有前景的抗癌剂被进一步探索。

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