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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.

Author information

1
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.
2
RCMI Cancer Research Center, Xavier University of Louisiana, New Orleans, LA 70125, USA.
3
Department of Chemistry, Xavier University of Louisiana, New Orleans, LA 70125, USA.
4
Jiangxi Provincial People's Hospital, Nanchang, 330006, China.
5
Department of Nuclear Medicine Affiliated Hospital, Luzhou Medical College, No. 25 Taiping Street, Luzhou, 646000, P. R. China.

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 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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