Synthesis, topoisomerase I inhibitory and cytotoxic activities of chromone derivatives
| Autor: | Jiraphun Jittikoon, Jiraporn Ungwitayatorn, Chirattikan Maicheen, Opa Vajragupta |
|---|---|
| Rok vydání: | 2012 |
| Předmět: |
Stereochemistry
Antineoplastic Agents Morin Pharmacology chemistry.chemical_compound Inhibitory Concentration 50 Structure-Activity Relationship Cell Line Tumor Drug Discovery medicine Cytotoxic T cell Humans IC50 biology Topoisomerase Molecular Docking Simulation chemistry Docking (molecular) Chromones Drug Design Chromone biology.protein Topoisomerase I Inhibitors Fisetin Camptothecin medicine.drug |
| Zdroj: | Medicinal chemistry (Shariqah (United Arab Emirates)). 9(3) |
| ISSN: | 1875-6638 |
| Popis: | A series of chromone derivatives were designed as potential topoisomerase I (Top I) inhibitors based on the docking simulation study. Sixteen synthesized compounds were evaluated for Top I inhibitory activity and some compounds were further tested for in vitro cytotoxic activity. The most potent inhibitor, chromone 11b showed greater inhibitory activity (IC50 = 1.46 μM) than the known Top I inhibitors, i.e., camptothecin, fisetin and morin, but inactive against breast cancer cell (MCF-7), oral cavity cancer cell (KB) and small cell lung cancer (NCI-H187). Chromone 11c, another potent inhibitor (IC50 = 6.16 μM), exhibited cytotoxic activity against KB (IC50 = 73.32 μM) and NCI-H187 (IC50 = 36.79 μM). |
| Databáze: | OpenAIRE |
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