Medicinal Chemistry

Synthesis and Biological Evaluation N-(6,7-dimethoxynaphthalen-yl) sulfamide Derivatives as Novel Inhibitors of Angiogenesis and Tumor Growth

Abstract

Guangsen Xu, Yi Zhou, Shengqiang Zhang, Shichao Ma, Fuming Xu, Hao Xu and Wenfang Xu

A novel series of N-(6,7-dimethoxynaphthalen-yl)sulfamide derivatives, targeting to angiogenesis and tumor growth, were well synthesized. Of these compounds, XGS-15 exhibited potent inhibitory effect on the proliferation of HCT116, PLC, U266, ES-2 and HEPG-2 cells and excellent anti-angiogenesis activity in both human umbilical vein endothelial cell (HUVEC) tube formation assay and the rat thoracic aorta rings test. Besides, compound XGS-15 showed weak inhibitory effects on human umbilical vein endothelial cell with high IC50 (>200 μM). So we speculated that compound XGS-15 revealed selective cytotoxic effect on tumor cells without influencing normal cells at low micromole ranges.