Fu Dong-Jun, Liu Ji-Feng, Zhao Ruo-Han, Li Jia-Huan, Zhang Sai-Yang, Zhang Yan-Bing
School of Pharmaceutical Sciences & Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou University, Zhengzhou 450001, China.
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China.
Molecules. 2017 Sep 5;22(9):1470. doi: 10.3390/molecules22091470.
A series of sulfanilamide-1,2,3-triazole hybrids were designed by a molecular hybridization strategy and evaluated for antiproliferative activity against three selected cancer cell lines (MGC-803, MCF-7 and PC-3). The detailed structure-activity relationships for these sulfanilamide-1,2,3-triazole hybrids were investigated. All these sulfanilamide-1,2,3-triazole hybrids exhibited moderate to potent activity against all cell lines. In particular 4-methyl--((1-(3-phenoxybenzyl)-1-1,2,3-triazol-4-yl)methyl)benzenesulfonamide () showed the most potent inhibitory effect against PC-3 cells, with an IC value of 4.08 μM. Furthermore, the tubulin polymerization inhibitory activity in vitro of compound was 2.41 μM. These sulfanilamide hybrids might serve as bioactive fragments for developing more potent antiproliferative agents.
通过分子杂交策略设计了一系列磺胺-1,2,3-三唑杂化物，并评估了它们对三种选定癌细胞系（MGC-803、MCF-7和PC-3）的抗增殖活性。研究了这些磺胺-1,2,3-三唑杂化物详细的构效关系。所有这些磺胺-1,2,3-三唑杂化物对所有细胞系均表现出中度至强效活性。特别是4-甲基-((1-(3-苯氧基苄基)-1H-1,2,3-三唑-4-基)甲基)苯磺酰胺（）对PC-3细胞显示出最有效的抑制作用，IC值为4.08μM。此外，化合物的体外微管蛋白聚合抑制活性为2.41μM。这些磺胺杂化物可能作为生物活性片段用于开发更有效的抗增殖剂。
