Synthesis, Molecular Docking Analysis and Biological Evaluations of Saccharide-Modified Thiadiazole Sulfonamide Derivatives
| Autor: | Zhen-Bin Han, Jian Wang, Yang Liu, Zuo-Peng Zhang, Hua-sheng Su, Ye Zhong, Maosheng Cheng, Lin Zhou |
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| Rok vydání: | 2021 |
| Předmět: |
0301 basic medicine
QH301-705.5 Cell Survival Carbohydrates Inhibitory postsynaptic potential Catalysis Article Polar surface area Inorganic Chemistry 03 medical and health sciences 0302 clinical medicine Cell Line Tumor Thiadiazoles Tumor Microenvironment Humans Viability assay Physical and Theoretical Chemistry Biology (General) Carbonic Anhydrase Inhibitors Molecular Biology QD1-999 Spectroscopy CA IX inhibitors Carbonic Anhydrases chemistry.chemical_classification Sulfonamides saccharide Chemistry Organic Chemistry tail approach Molecular Docking Analysis General Medicine Combinatorial chemistry Computer Science Applications Sulfonamide Molecular Docking Simulation 030104 developmental biology pH of the tumor cell microenvironment Cell culture 030220 oncology & carcinogenesis Enzyme inhibitory HT29 Cells Human cancer |
| Zdroj: | International Journal of Molecular Sciences International Journal of Molecular Sciences, Vol 22, Iss 5482, p 5482 (2021) Volume 22 Issue 11 |
| ISSN: | 1422-0067 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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