Design, synthesis and biological evaluation of quinoline amide derivatives as novel VEGFR-2 inhibitors

Y Yang, L Shi, Y Zhou, HQ Li, ZW Zhu…

Index: Yang, Ying; Shi, Lei; Zhou, Yang; Li, Huan-Qiu; Zhu, Zhen-Wei; Zhu, Hai-Liang Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 22 p. 6653 - 6656

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Citation Number: 39

Abstract

Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a crucial role in the process of cancer angiogenesis. A series of quinoline amide derivatives were prepared and found to be good inhibitors of VEGFR-2. The inhibitory activities were investigated against VEGFR-2 kinase and human umbilical vein endothelial cells (HUVEC) in vitro. Compound 6 (5-chloro- 2-hydroxy-N-(quinolin-8-yl) benzamide) exhibited the most potent inhibitory activity (IC50= ...