Synthesis and cytotoxicity of novel 4-(4-(substituted)-1H-1,2,3-triazol-1-yl)-N-phenethylbenzenesulfonamides

被引：0
|
作者：
Ratchanok Pingaew
Supaluk Prachayasittikul
Somsak Ruchirawat
Virapong Prachayasittikul
机构：
[1] Srinakharinwirot University,Department of Chemistry, Faculty of Science
[2] Mahidol University,Center of Data Mining and Biomedical Informatics, Faculty of Medical Technology
[3] Chulabhorn Research Institute,Laboratory of Medicinal Chemistry
[4] Chulabhorn Graduate Institute,Program in Chemical Biology
[5] Ministry of Education,Center of Excellence on Environmental Health and Toxicology, Commission on Higher Education (CHE)
[6] Mahidol University,Department of Clinical Microbiology and Applied Technology, Faculty of Medical Technology
来源：
Medicinal Chemistry Research | 2014年 / 23卷
关键词：
Sulfonamide; Triazole; Click reaction; Cytotoxicity;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
A new series of 4-(4-(substituted)-1H-1,2,3-triazol-1-yl)-N-phenethylbenzenesulfonamide derivatives 5 were synthesized through the Click approach and evaluated for their cytotoxic activity against four cancer cell lines (HuCCA-1, HepG2, A549, and MOLT-3). Most of the synthesized triazoles 5 displayed cytotoxicity against MOLT-3 cell line, except for analogs 5a–c and 5e. Significantly, 4-phenyltriazoles (5a and 5n), 4-(naphthalen-2-yloxy)methyltriazole 5d, as well as 4-((2-oxo-2H-chromen-7-yl)oxy)methyltriazole 5l showed higher cytotoxic activity against HepG2 cells than the reference drug, etoposide. Interestingly, the 4-phenyltriazole 5a was the most potent and promising compound with IC50 value of 9.07 μM against HepG2 cell line. The analog 5a also exerted the highest cytotoxic activity against HuCCA-1 cells. This finding provides the novel lead molecules for further development.
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页码：1768 / 1780
页数：12
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