Derivatives of 1,2,4-triazole imines acting as dual iNOS and tumor cell growth inhibitors
| Autor: | Thomas M. Finetti, Jeffrey Wisnoski, Christophe Guillon, Diane E. Heck, Peter Warren DeMatteo, Anna M. Vetrano, Jaya Saxena, Angela Hunter, Ned D. Heindel, Geraldine Verderone, Jeffrey D. Laskin, Robert D. Rapp, Laurie B. Joseph |
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| Rok vydání: | 2020 |
| Předmět: |
Triazole
Nitric Oxide Synthase Type II Antineoplastic Agents Nitric Oxide 01 natural sciences Biochemistry Article Nitric oxide HeLa Mice Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Animals Potency Cytotoxicity Molecular Biology Cells Cultured Cell Proliferation Dose-Response Relationship Drug Molecular Structure biology 010405 organic chemistry Organic Chemistry 1 2 4-Triazole Triazoles biology.organism_classification Growth Inhibitors 0104 chemical sciences Nitric oxide synthase 010404 medicinal & biomolecular chemistry chemistry biology.protein Imines Drug Screening Assays Antitumor Growth inhibition |
| Zdroj: | Bioorg Chem |
| ISSN: | 0045-2068 |
| DOI: | 10.1016/j.bioorg.2020.104128 |
| Popis: | A set of 4-(R(2)-imino)-3-mercapto-5-(R(1))-4H-1,2,4-triazoles derivatives were synthesized, characterized and evaluated for their ability to inhibit nitric oxide (NO) production in PAM212 mouse keratinocytes, which led to the discovery and the subsequent evaluation of their growth inhibitory cytotoxic potency toward that same mouse cell line together with a number of human cells lines (PC3, HT-29 and HeLa). Some limited SAR could be established for both NO production inhibition potency and growth inhibition cytotoxicity. Noticeably, the compounds designed to be nitrofurantoin mimics were the most potent anti-neoplastic agents. |
| Databáze: | OpenAIRE |
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