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Design, synthesis and biological evaluation of pazopanib derivatives as antitumor agents
Yuping Jia1, Jian Zhang, Jinhong Feng
1Shandong 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.
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