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

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

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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.
Department of Chemistry, Xavier University of Louisiana, New Orleans, LA 70125, USA.
Jiangxi Provincial People's Hospital, Nanchang, 330006, China.
Department of Nuclear Medicine Affiliated Hospital, Luzhou Medical College, No. 25 Taiping Street, Luzhou, 646000, P. R. China.


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.

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