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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-other | 2017 Oct

REPOSITORIES: biostudies-other

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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)-1<i>H</i>-1,2,3-triazol-1-yl)phenoxy)-<i>N</i>-methylpicolinamide (<b>8f</b>) potently suppressed the proliferation of HT-29 cancer cells by inducing apoptos  ...[more]

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