title: Synthesis, topoisomerase I inhibitory and cytotoxic activities of chromone derivatives.
abstract: 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).
authors.affiliation: Faculty of Pharmacy, Mahidol University, Bangkok, Thailand.
authors.forename: Chirattikan
authors.initials: C
authors.lastname: Maicheen
authors.forename: Jiraphun
authors.initials: J
authors.lastname: Jittikoon
authors.forename: Opa
authors.initials: O
authors.lastname: Vajragupta
authors.forename: Jiraporn
authors.initials: J
authors.lastname: Ungwitayatorn
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D045744:Cell Line, Tumor; D002867:Chromones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D062105:Molecular Docking Simulation; D013329:Structure-Activity Relationship; D059004:Topoisomerase I Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000970:Antineoplastic Agents; D002867:Chromones; D059004:Topoisomerase I Inhibitors