Journal
CHEMICAL BIOLOGY & DRUG DESIGN
Volume 83, Issue 3, Pages 306-316Publisher
WILEY-BLACKWELL
DOI: 10.1111/cbdd.12243
Keywords
anti-angiogenesis; antitumor agent; pazopanib derivatives; synthesis
Funding
- Ph.D. Programs Foundation of Ministry of Education of P.R. China [20110131110037]
- The Shandong Provincial Natural Science Foundation, China [ZR2010CQ034]
- The National Natural Science Foundation of China [21172134]
- National High Technology Research and Development Program of China [2011ZX09401-015]
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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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