Efficient Synthesis and Biological Activity of Novel Indole Derivatives as VEGFR-2 Tyrosine Kinase Inhibitors

作者：C. Zhang, Dongpo Xu, J. Wang, Congmin Kang · 发表于：Russian Journal of General Chemistry · 年份：2017 · DOI：10.1134/s1070363217120465 · 被引用次数：24 · 研究领域：Angiogenesis and VEGF in Cancer、HER2/EGFR in Cancer Research、Synthesis and biological activity

A series of novel indole derivatives were synthesized as potent inhibitors for the vascular endothelial growth factor receptor 2 (VEGFR-2) tyrosine kinase. Among those, compound 10b demonstrated the highest growth inhibition rate of 66.7% against the VEGFR-2 tyrosine kinase at 10 μM which indicates that indole-benzothiazole might be the favorable structure. The binding mode of compound 10b with VEGFR-2 tyrosine kinase was evaluated by molecular docking.