Synthesis and Antitumor Activity of Triazole-Containing Sorafenib Analogs

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 ag...

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Detalles Bibliográficos
Autores principales: Ye, Wenjing, Yao, Qi, Yu, Simiao, Gong, Ping, Qin, Mingze
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6151694/
https://www.ncbi.nlm.nih.gov/pubmed/29064424
http://dx.doi.org/10.3390/molecules22101759
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author Ye, Wenjing
Yao, Qi
Yu, Simiao
Gong, Ping
Qin, Mingze
author_facet Ye, Wenjing
Yao, Qi
Yu, Simiao
Gong, Ping
Qin, Mingze
author_sort Ye, Wenjing
collection PubMed
description 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.
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spelling pubmed-61516942018-11-13 Synthesis and Antitumor Activity of Triazole-Containing Sorafenib Analogs Ye, Wenjing Yao, Qi Yu, Simiao Gong, Ping Qin, Mingze Molecules Article 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. MDPI 2017-10-24 /pmc/articles/PMC6151694/ /pubmed/29064424 http://dx.doi.org/10.3390/molecules22101759 Text en © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Ye, Wenjing
Yao, Qi
Yu, Simiao
Gong, Ping
Qin, Mingze
Synthesis and Antitumor Activity of Triazole-Containing Sorafenib Analogs
title Synthesis and Antitumor Activity of Triazole-Containing Sorafenib Analogs
title_full Synthesis and Antitumor Activity of Triazole-Containing Sorafenib Analogs
title_fullStr Synthesis and Antitumor Activity of Triazole-Containing Sorafenib Analogs
title_full_unstemmed Synthesis and Antitumor Activity of Triazole-Containing Sorafenib Analogs
title_short Synthesis and Antitumor Activity of Triazole-Containing Sorafenib Analogs
title_sort synthesis and antitumor activity of triazole-containing sorafenib analogs
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6151694/
https://www.ncbi.nlm.nih.gov/pubmed/29064424
http://dx.doi.org/10.3390/molecules22101759
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