ACS Medicinal Chemistry Letters p. 592 - 597 (2014)
Update date:2022-08-03
Topics:
Lv, Yongcong
Li, Mengyuan
Liu, Ting
Tong, Linjiang
Peng, Ting
Wei, Lixin
Ding, Jian
Xie, Hua
Duan, Wenhu
Inhibition of VEGFR-2 signaling pathway has already become one of the most promising approaches for the treatment of cancer. In this study, we describe the design, synthesis, and biological evaluation of a new series of naphthamides as potent inhibitors of VEGFR-2. Among these compounds, 14c exhibited high VEGFR-2 inhibitory potency in both enzymatic and HUVEC cellular proliferation assays, with IC50 values of 1.5 and 0.9 nM, respectively. Kinase selectivity profiling revealed that 14c was a multitargeted inhibitor, and it also exhibited good potency against VEGFR-1, PDGFR-β, and RET. Furthermore, 14c effectively blocked tube formation of HUVEC at nanomolar level. Overall, 14c might be a promising candidate for the treatment of cancer.
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