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

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.

SUBMITTER: Gu L

PROVIDER: S-EPMC6364840 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature

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

Gu Linghui L Wang Peng P Zhong Qiu Q Deng Yuxing Y Xie Jiangping J Liu Fei F Xiao Fan F Zheng Shilong S Chen Yue Y Wang Guangdi G He Ling L

RSC advances 20170130 16

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 <b>1p</b> 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 ...[more]

PMID: 30740218

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