Synthesis and Biological Evaluation N-(6,7-dimethoxynaphthalen-yl) sulfamide Derivatives as Novel Inhibitors of Angiogenesis and Tumor GrowthGuangsen Xu1, Yi Zhou1, Shengqiang Zhang1, Shichao Ma1, Fuming Xu1, Hao Xu2* and Wenfang Xu1*
- *Corresponding Author:
- Wenfang Xu
Department of Medicinal Chemistry
School of Pharmaceutical Science, Shandong University
44 West Wenhua Road, Ji’nan, Shandong 250012, P.R. China
Tel/Fax: +86 531 88382264
Department of Breast and Thyroid Surgery
Shandong Provincial Hospital Affiliated to Shandong University
324 Jingwu-Weiqi Road, Ji’nan 250021, P.R. China
Received date: July 05, 2014; Accepted date: August 11, 2014; Published date: August 11, 2014
Citation: Xu G, Zhou Y, Zhang S, Ma S, Xu F, et al. (2014) Synthesis and Biological Evaluation N-(6,7-dimethoxynaphthalen-yl) sulfamide Derivatives as Novel Inhibitors of Angiogenesis and Tumor Growth. Med chem 4:598-605. doi:10.4172/2161-0444.1000200
Copyright: © 2014 Xu G, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
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.