Sulfonylguanidine Derivatives as Potential Antimelanoma Agents
| Autor: | Stéphane Rocchi, Nedra Hamouda-Tekaya, Cyril Ronco, Tom Baladi, Rachid Benhida, Leticia Christina Pires Gonçalves |
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| Rok vydání: | 2020 |
| Předmět: |
Skin Neoplasms
Cell Survival Tumor cells Antineoplastic Agents 01 natural sciences Biochemistry Sulfonylguanidine Structure-Activity Relationship Cell Line Tumor Drug Discovery medicine Humans General Pharmacology Toxicology and Pharmaceutics Melanoma Guanidine derivatives Guanidine Cell Proliferation Pharmacology chemistry.chemical_classification Sulfonyl Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Organic Chemistry Hydrogen-Ion Concentration medicine.disease Combinatorial chemistry 0104 chemical sciences Sulfonamide Molecular Docking Simulation 010404 medicinal & biomolecular chemistry chemistry Molecular Medicine Cancer cell lines Drug Screening Assays Antitumor Function (biology) |
| Zdroj: | ChemMedChem. 15(13) |
| ISSN: | 1860-7187 |
| Popis: | Sulfonylguanidines are interesting bioactive compounds with a broad range of applications in the treatment of different pathologies. 2-Aminobenzazole-based structures are well employed in the development of new anticancer drugs. Two series of novel N-benzazol-2-yl-N'-sulfonyl guanidine derivatives were synthesized with the sulfonylguanidine in either an extra- or intracyclic frame. They were evaluated for their antiproliferative activity against malignant melanoma tumor cells, thus allowing structure-activity relationships to be defined. Additionally, NCI-60 screening was performed for the best analogue to study its efficiency against a panel of other cancer cell lines. The stability profile of this promising compound was then validated. During the synthetic process, an unexpected new deamidination of the sulfonylguanidine towards sulfonamide function was also identified. |
| Databáze: | OpenAIRE |
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