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Synthesis and Biological Evaluation N-(6,7-dimethoxynaphthalen-yl) sulfamide Derivatives as Novel Inhibitors of Angiogenesis and Tumor Growth | OMICS International | Abstract
ISSN: 2161-0444

Medicinal Chemistry
Open Access

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Research Article

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

Guangsen Xu1, Yi Zhou1, Shengqiang Zhang1, Shichao Ma1, Fuming Xu1, Hao Xu2* and Wenfang Xu1*

1Department of Medicinal Chemistry, School of Pharmaceutical Science, Shandong University, 44 West Wenhua Road, Ji’nan, Shandong 250012, P.R. China

2Department of Breast and Thyroid Surgery, Shandong Provincial Hospital Affiliated to Shandong University, 324 Jingwu-Weiqi Road, Ji’nan 250021, P.R. China

*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
E-mail: [email protected]

Hao Xu
Department of Breast and Thyroid Surgery
Shandong Provincial Hospital Affiliated to Shandong University
324 Jingwu-Weiqi Road, Ji’nan 250021, P.R. China
E-mail: [email protected]

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.

Abstract

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.

Keywords

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