Synthesis,Molecular Docking Analysis and Biological Evaluations of Saccharide-Modified Thiadiazole Sulfonamide Derivatives |
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| Authors: | Zuo-Peng Zhang Ye Zhong Zhen-Bin Han Lin Zhou Hua-Sheng Su Jian Wang Yang Liu Mao-Sheng Cheng |
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| Affiliation: | Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China; (Z.-P.Z.); (Y.Z.); (Z.-B.H.); (L.Z.); (H.-S.S.); (J.W.) |
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| Abstract: | A series of saccharide-modified thiadiazole sulfonamide derivatives has been designed and synthesized by the “tail approach” and evaluated for inhibitory activity against carbonic anhydrases II, IX, and XII. Most of the compounds showed high topological polar surface area (TPSA) values and excellent enzyme inhibitory activity. The impacts of some compounds on the viability of HT-29, MDA-MB-231, and MG-63 human cancer cell lines were examined under both normoxic and hypoxic conditions, and they showed certain inhibitory effects on cell viability. Moreover, it was found that the series of compounds had the ability to raise the pH of the tumor cell microenvironment. All the results proved that saccharide-modified thiadiazole sulfonamides have important research prospects for the development of CA IX inhibitors. |
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| Keywords: | saccharide tail approach pH of the tumor cell microenvironment CA IX inhibitors |
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