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Synthesis and Antitumor Activity of Triazole-Containing Sorafenib Analogs.

ABSTRACT: 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.

SUBMITTER: Ye W

PROVIDER: S-EPMC6151694 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature

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Synthesis and Antitumor Activity of Triazole-Containing Sorafenib Analogs.

Ye Wenjing W Yao Qi Q Yu Simiao S Gong Ping P Qin Mingze M

Molecules (Basel, Switzerland) 20171024 10

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 apoptos ...[more]

PMID: 29064424

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