Synthesis and biological evaluation of novel pazopanib derivatives as antitumor agents

H Qi, L Chen, B Liu, X Wang, L Long, D Liu

Index: Qi, Haofei; Chen, Ligong; Liu, Bingni; Wang, Xinran; Long, Li; Liu, Dengke Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 4 p. 1108 - 1110

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Citation Number: 3

Abstract

Abstract A series of novel pazopanib derivatives, 7a–m, were designed and synthesized by modification of terminal benzene and indazole rings in pazopanib. The structures of all the synthesized compounds were confirmed by 1 H NMR and MS. Their inhibitory activity against VEGFR-2, PDGFR-α and c-kit tyrosine kinases were evaluated. All the compounds exhibited definite kinase inhibition, in which compound 7l was most potent with IC 50 ...