S ‐(4‐Methoxyphenyl)‐4‐methoxybenzenesulfonothioate as a Promising Lead Compound for the Development of a Renal Carcinoma Agent
| العنوان: | S ‐(4‐Methoxyphenyl)‐4‐methoxybenzenesulfonothioate as a Promising Lead Compound for the Development of a Renal Carcinoma Agent |
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| المؤلفون: | Adilson Beatriz, Murilo K. A. Yonekawa, Camilla I. Nantes, Maria de Fatima Cepa Matos, Ruoli Bai, Ernest Hamel, Dênis Pires de Lima, Rodrigo Juliano Oliveira, Edson dos Anjos dos Santos, Renata Trentin Perdomo, James C. Burnett, Ingrid D. Pereira, Danielle Bogo |
| المصدر: | ChemMedChem. 15:449-458 |
| بيانات النشر: | Wiley, 2020. |
| سنة النشر: | 2020 |
| مصطلحات موضوعية: | Cell, Antineoplastic Agents, Caspase 3, 01 natural sciences, Biochemistry, Cell Line, Polymerization, Mice, Tubulin, Drug Discovery, medicine, Animals, Humans, Cytotoxic T cell, General Pharmacology, Toxicology and Pharmaceutics, Carcinoma, Renal Cell, Cell Proliferation, Pharmacology, Molecular Structure, biology, 010405 organic chemistry, Chemistry, Endoplasmic reticulum, Organic Chemistry, Molecular biology, Kidney Neoplasms, 0104 chemical sciences, Molecular Docking Simulation, 010404 medicinal & biomolecular chemistry, medicine.anatomical_structure, Apoptosis, Cell culture, Unfolded protein response, biology.protein, Molecular Medicine, Drug Screening Assays, Antitumor |
| الوصف: | Organosulfur compounds show cytotoxic potential towards many tumor cell lines. Disulfides and thiosulfonates act through apoptotic processes, inducing proteins associated with apoptosis, endoplasmic reticulum stress, and the unfolded protein response. Three p-substituted symmetric diaryl disulfides and three diaryl thiosulfonates were synthesized and analyzed for inhibition of tubulin polymerization and for human cancer cell cytotoxic activity against seven tumor cell lines and a non-tumor cell line. S-(4-methoxyphenyl)-4-methoxybenzenesulfonothioate (6) exhibited inhibition of tubulin polymerization and showed the best antiproliferative potential, especially against the 786-0 cell line, being six times more selective as compared with the non-tumor cell line. In addition, compound 6 was able to activate caspase-3 after 24 and 48 h treatments of the 786-0 cell line and induced cell-cycle arrest in the G2/M stage at the highest concentration evaluated at 24 and 48 h. Compound 6 was able to cause complete inhibition of proliferation, inducing the death of 786-0 cells, by increasing the number of cells at G2/M and greater activation of caspase-3. |
| تدمد: | 1860-7187 1860-7179 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9b0f1082b9dca8b00da011f886d5e5d0 https://doi.org/10.1002/cmdc.201900566 |
| حقوق: | CLOSED |
| رقم الأكسشن: | edsair.doi.dedup.....9b0f1082b9dca8b00da011f886d5e5d0 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 18607187 18607179 |
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