Discovery of novel picolinamide-based derivatives as novel VEGFR-2 kinase inhibitors: synthesis, in vitro biological evaluation and molecular docking

作者：Sun, Wuji; Fang, Shubiao; Yan, Hong^*

来源：Medchemcomm, 2018, 9(6): 1054-1058.

DOI：10.1039/c8md00057c

• ENDOTHELIAL GROWTH-FACTOR
• COLORECTAL-CANCER
• RECEPTOR
• DESIGN

Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a crucial role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has emerged as an attractive target for cancer therapy. In our effort, a novel series of picolinamide-based derivatives were designed and synthesized as potent and effective VEGFR-2 inhibitors. All the newly prepared compounds were evaluated in vitro for their antiproliferative activity against A549 and HepG2 cell lines. Among the new compounds, 8j and 8l exhibited better activity against both A549 and HepG2 cell lines. Molecular docking was performed to investigate the binding capacity and binding mode with VEGFR-2 (PDB code: ; 4ASD).

• 出版日期2018-6-1
• 单位北京工业大学