Design, Synthesis, and Biological Evaluation of Axitinib Derivatives
Axitinib is an approved kinase inhibitor for the therapy of advanced metastatic renal cell carcinoma (RCC). It prevents angiogenesis, cellular adhesion, and induces apoptosis of cancer cells. Here, nine axitinib derivatives were designed by replacing the C=C moiety with the N=N group, and the substi...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017704/ https://www.ncbi.nlm.nih.gov/pubmed/29570686 http://dx.doi.org/10.3390/molecules23040747 |
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author | Wei, Na Liang, Jianqing Peng, Shengming Sun, Qiang Dai, Qiuyun Dong, Mingxin |
author_facet | Wei, Na Liang, Jianqing Peng, Shengming Sun, Qiang Dai, Qiuyun Dong, Mingxin |
author_sort | Wei, Na |
collection | PubMed |
description | Axitinib is an approved kinase inhibitor for the therapy of advanced metastatic renal cell carcinoma (RCC). It prevents angiogenesis, cellular adhesion, and induces apoptosis of cancer cells. Here, nine axitinib derivatives were designed by replacing the C=C moiety with the N=N group, and the substituted benzene or pyrrole analogs were considered to replace the pyridine ring. Biological activity results showed that most of nascent derivatives exhibited favorable VEGFR-2 kinase inhibitory activities, and TM6, 7, 9, and 11 behaved more potent anti-proliferative activities than axitinib. This novel series of compounds shows a potential for the treatment of solid tumors and other diseases where angiogenesis plays an important role. |
format | Online Article Text |
id | pubmed-6017704 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-60177042018-11-13 Design, Synthesis, and Biological Evaluation of Axitinib Derivatives Wei, Na Liang, Jianqing Peng, Shengming Sun, Qiang Dai, Qiuyun Dong, Mingxin Molecules Article Axitinib is an approved kinase inhibitor for the therapy of advanced metastatic renal cell carcinoma (RCC). It prevents angiogenesis, cellular adhesion, and induces apoptosis of cancer cells. Here, nine axitinib derivatives were designed by replacing the C=C moiety with the N=N group, and the substituted benzene or pyrrole analogs were considered to replace the pyridine ring. Biological activity results showed that most of nascent derivatives exhibited favorable VEGFR-2 kinase inhibitory activities, and TM6, 7, 9, and 11 behaved more potent anti-proliferative activities than axitinib. This novel series of compounds shows a potential for the treatment of solid tumors and other diseases where angiogenesis plays an important role. MDPI 2018-03-23 /pmc/articles/PMC6017704/ /pubmed/29570686 http://dx.doi.org/10.3390/molecules23040747 Text en © 2018 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 Wei, Na Liang, Jianqing Peng, Shengming Sun, Qiang Dai, Qiuyun Dong, Mingxin Design, Synthesis, and Biological Evaluation of Axitinib Derivatives |
title | Design, Synthesis, and Biological Evaluation of Axitinib Derivatives |
title_full | Design, Synthesis, and Biological Evaluation of Axitinib Derivatives |
title_fullStr | Design, Synthesis, and Biological Evaluation of Axitinib Derivatives |
title_full_unstemmed | Design, Synthesis, and Biological Evaluation of Axitinib Derivatives |
title_short | Design, Synthesis, and Biological Evaluation of Axitinib Derivatives |
title_sort | design, synthesis, and biological evaluation of axitinib derivatives |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017704/ https://www.ncbi.nlm.nih.gov/pubmed/29570686 http://dx.doi.org/10.3390/molecules23040747 |
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