These authers contributed equally to this work.
Design, Synthesis and Biological Evaluation of Pazopanib Derivatives as Antitumor Agents
Article first published online: 1 FEB 2014
© 2013 John Wiley & Sons A/S.
Chemical Biology & Drug Design
Volume 83, Issue 3, pages 306–316, March 2014
How to Cite
Jia, Y., Zhang, J., Feng, J., Xu, F., Pan, H. and Xu, W. (2014), Design, Synthesis and Biological Evaluation of Pazopanib Derivatives as Antitumor Agents. Chemical Biology & Drug Design, 83: 306–316. doi: 10.1111/cbdd.12243
- Issue published online: 25 FEB 2014
- Article first published online: 1 FEB 2014
- Accepted manuscript online: 11 OCT 2013 03:17AM EST
- Manuscript Accepted: 27 SEP 2013
- Manuscript Revised: 22 SEP 2013
- Manuscript Received: 2 JUL 2013
- Foundation of Ministry of Education. Grant Number: 20110131110037
- The Shandong Provincial Natural Science Foundation. Grant Number: ZR2010CQ034
- The National Natural Science Foundation. Grant Number: 21172134
- National High Technology Research and Development Program. Grant Number: 2011ZX09401-015
- antitumor agent;
- pazopanib derivatives;
A novel series of pazopanib derivatives were designed, synthesized, and evaluated for their inhibitory activity against a series of kinases including VEGFR-2, EGFR, AKT1, ALK1, and ABL1. The anti-angiogenic activities ex vivo of some compounds were also investigated. Compounds P2d and P2e demonstrated outstanding inhibitory activity against VEGFR-2 and ABL1 and higher anti-angiogenic activity compared with Pazopanib, the reference standard. These two compounds (P2d and P2e) could be used as novel lead compounds for further development of anticancer agents.