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Open AccessArticle

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
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Molecules 2017, 22(10), 1759; https://doi.org/10.3390/molecules22101759
Received: 20 September 2017 / Revised: 13 October 2017 / Accepted: 15 October 2017 / Published: 24 October 2017
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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MDPI and ACS Style

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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