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Molecules 2017, 22(9), 1470; doi:10.3390/molecules22091470

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

1
School of Pharmaceutical Sciences & Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou University, Zhengzhou 450001, China
2
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Received: 21 July 2017 / Revised: 21 August 2017 / Accepted: 31 August 2017 / Published: 5 September 2017
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Abstract

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-(3-phenoxybenzyl)-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 μM. Furthermore, the tubulin polymerization inhibitory activity in vitro of compound 11f was 2.41 μM. These sulfanilamide hybrids might serve as bioactive fragments for developing more potent antiproliferative agents. View Full-Text
Keywords: sulfanilamide-1,2,3-triazole; molecular hybridization strategy; antiproliferative activity; structure-activity relationships; tubulin polymerization sulfanilamide-1,2,3-triazole; molecular hybridization strategy; antiproliferative activity; structure-activity relationships; tubulin polymerization
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MDPI and ACS Style

Fu, D.-J.; Liu, J.-F.; Zhao, R.-H.; Li, J.-H.; Zhang, S.-Y.; Zhang, Y.-B. Design and Antiproliferative Evaluation of Novel Sulfanilamide Derivatives as Potential Tubulin Polymerization Inhibitors. Molecules 2017, 22, 1470.

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