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

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 ?M. Furthermore, the tubulin polymerization inhibitory activity in vitro of compound 11f was 2.41 ?M. These sulfanilamide hybrids might serve as bioactive fragments for developing more potent antiproliferative agents.

SUBMITTER: Fu DJ

PROVIDER: S-EPMC6151726 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature

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

Fu Dong-Jun DJ Liu Ji-Feng JF Zhao Ruo-Han RH Li Jia-Huan JH Zhang Sai-Yang SY Zhang Yan-Bing YB

Molecules (Basel, Switzerland) 20170905 9

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-<i>N</i>-((1-(3-phenoxybenzyl)-1<i>H</i>-1 ...[more]

PMID: 28872607

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