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Chem Biol Drug Des. 2014 Mar;83(3):306-16. doi: 10.1111/cbdd.12243. Epub 2014 Feb 1.

Design, synthesis and biological evaluation of pazopanib derivatives as antitumor agents.

Author information

1
Shandong Institute of Pharmaceutical Industry, Ji'nan, Shandong, 250101, China.

Abstract

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.

KEYWORDS:

anti-angiogenesis; antitumor agent; pazopanib derivatives; synthesis

PMID:
24119291
DOI:
10.1111/cbdd.12243
[Indexed for MEDLINE]

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