Design and Antiproliferative Evaluation of Novel Sulfanilamide Derivatives as Potential Tubulin Polymerization Inhibitors

作者：Fu, Dong-Jun; Liu, Ji-Feng; Zhao, Ruo-Han; Li, Jia-Huan; Zhang, Sai-Yang^*; Zhang, Yan-Bing^*

来源：Molecules, 2017, 22(9): 1470.

DOI：10.3390/molecules22091470

• sulfanilamide-1,2,3-triazole
• molecular hybridization strategy
• antiproliferative activity
• structure-activity relationships
• tubulin polymerization

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-N-((1-(3phenoxybenzyl)-1H-1,2,3-triazol-4-yl) methyl) benzenesulfonamide (11f) showed the most potent inhibitory effect against PC-3 cells, with an IC50 value of 4.08 mu M. Furthermore, the tubulin polymerization inhibitory activity in vitro of compound 11f was 2.41 mu M. These sulfanilamide hybrids might serve as bioactive fragments for developing more potent antiproliferative agents.

• 出版日期2017-9
• 单位郑州大学