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Design, Synthesis and Biological Evaluation of Pazopanib Derivatives as Antitumor Agents
Author(s) -
Jia Yuping,
Zhang Jian,
Feng Jinhong,
Xu Fuming,
Pan Huili,
Xu Wenfang
Publication year - 2014
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12243
Subject(s) - pazopanib , pharmacology , computational biology , chemistry , combinatorial chemistry , biology , medicine , cancer , sunitinib
A novel series of pazopanib derivatives were designed, synthesized, and evaluated for their inhibitory activity against a series of kinases including VEGFR ‐2, EGFR , AKT 1, ALK 1, and ABL 1. The anti‐angiogenic activities ex vivo of some compounds were also investigated. Compounds P2d and P2e demonstrated outstanding inhibitory activity against VEGFR ‐2 and ABL 1 and higher anti‐angiogenic activity compared with P azopanib, the reference standard. These two compounds ( P2d and P2e ) could be used as novel lead compounds for further development of anticancer agents.