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...

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Main Authors:	Na Wei, Jianqing Liang, Shengming Peng, Qiang Sun, Qiuyun Dai, Mingxin Dong
Format:	Article
Language:	English
Published:	MDPI AG 2018-03-01
Series:	Molecules
Subjects:	axitinib synthesis VEGFR-2 inhibitor tumor
Online Access:	http://www.mdpi.com/1420-3049/23/4/747

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spelling	doaj-28a90f9d794b43e7807b94528df3b4822020-11-24T23:52:07ZengMDPI AGMolecules1420-30492018-03-0123474710.3390/molecules23040747molecules23040747Design, Synthesis, and Biological Evaluation of Axitinib DerivativesNa Wei0Jianqing Liang1Shengming Peng2Qiang Sun3Qiuyun Dai4Mingxin Dong5Department of Chemistry, Xiangtan University, Xiangtan 411105, ChinaLab of Protein Engineering, Beijing Institute of Biotechnology, Beijing 100071, ChinaDepartment of Chemistry, Xiangtan University, Xiangtan 411105, ChinaLab of Protein Engineering, Beijing Institute of Biotechnology, Beijing 100071, ChinaLab of Protein Engineering, Beijing Institute of Biotechnology, Beijing 100071, ChinaLab of Protein Engineering, Beijing Institute of Biotechnology, Beijing 100071, ChinaAxitinib 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.http://www.mdpi.com/1420-3049/23/4/747axitinibsynthesisVEGFR-2inhibitortumor
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Na Wei Jianqing Liang Shengming Peng Qiang Sun Qiuyun Dai Mingxin Dong
spellingShingle	Na Wei Jianqing Liang Shengming Peng Qiang Sun Qiuyun Dai Mingxin Dong Design, Synthesis, and Biological Evaluation of Axitinib Derivatives Molecules axitinib synthesis VEGFR-2 inhibitor tumor
author_facet	Na Wei Jianqing Liang Shengming Peng Qiang Sun Qiuyun Dai Mingxin Dong
author_sort	Na Wei
title	Design, Synthesis, and Biological Evaluation of Axitinib Derivatives
title_short	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_sort	design, synthesis, and biological evaluation of axitinib derivatives
publisher	MDPI AG
series	Molecules
issn	1420-3049
publishDate	2018-03-01
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.
topic	axitinib synthesis VEGFR-2 inhibitor tumor
url	http://www.mdpi.com/1420-3049/23/4/747
work_keys_str_mv	AT nawei designsynthesisandbiologicalevaluationofaxitinibderivatives AT jianqingliang designsynthesisandbiologicalevaluationofaxitinibderivatives AT shengmingpeng designsynthesisandbiologicalevaluationofaxitinibderivatives AT qiangsun designsynthesisandbiologicalevaluationofaxitinibderivatives AT qiuyundai designsynthesisandbiologicalevaluationofaxitinibderivatives AT mingxindong designsynthesisandbiologicalevaluationofaxitinibderivatives
_version_	1725474811189133312

Design, Synthesis, and Biological Evaluation of Axitinib Derivatives

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