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Synthesis, Topoisomerase I Inhibitory and Cytotoxic Activities of Chromone Derivatives

[ Vol. 9 , Issue. 3 ]


Chirattikan Maicheen, Jiraphun Jittikoon, Opa Vajragupta and Jiraporn Ungwitayatorn   Pages 329 - 339 ( 11 )


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).


Chromone derivatives, topoisomerase I inhibitory activity, cytotoxic activity, enzymes, DNA, flavonoids, hydrogen bonds, melting points, dimethylsulfoxide, chromatography


Faculty of Pharmacy, Mahidol University, 447 Sri-Ayudhya Road, Bangkok 10400, Thailand.

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