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Molecules 2017, 22(10), 1759;

Synthesis and Antitumor Activity of Triazole-Containing Sorafenib Analogs

Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education, 103 Wenhua Road, Shenyang 110016, China
Author to whom correspondence should be addressed.
Received: 20 September 2017 / Revised: 13 October 2017 / Accepted: 15 October 2017 / Published: 24 October 2017
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Using a highly effective binuclear Cu complex as the catalyst, the 1,3-dipolar cycloaddition reactions between 16 alkynes and two azides were successfully performed and resulted in the production of 25 new triazole-containing sorafenib analogs. Several compounds were evaluated as potent antitumor agents. Among them, 4-(4-(4-(3-fluorophenyl)-1H-1,2,3-triazol-1-yl)phenoxy)-N-methylpicolinamide (8f) potently suppressed the proliferation of HT-29 cancer cells by inducing apoptosis and almost completely inhibited colony formation at a low micromolar concentration. View Full-Text
Keywords: binuclear Cu catalyst; sorafenib analogs; antitumor agents binuclear Cu catalyst; sorafenib analogs; antitumor agents

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Ye, W.; Yao, Q.; Yu, S.; Gong, P.; Qin, M. Synthesis and Antitumor Activity of Triazole-Containing Sorafenib Analogs. Molecules 2017, 22, 1759.

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