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


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Abstract

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.

About the authors

C. Zhang

College of Chemical Engineering

Email: lvyingtao@qust.edu.cn
China, Qingdao, 266042

D. Xu

College of Chemical Engineering

Email: lvyingtao@qust.edu.cn
China, Qingdao, 266042

J. Wang

College of Chemical Engineering

Email: lvyingtao@qust.edu.cn
China, Qingdao, 266042

C. Kang

College of Chemical Engineering

Author for correspondence.
Email: lvyingtao@qust.edu.cn
China, Qingdao, 266042


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