Synthesis, Topoisomerase I Inhibitory and Cytotoxic Activities of Chromone Derivatives

Author(s): Chirattikan Maicheen, Jiraphun Jittikoon, Opa Vajragupta, Jiraporn Ungwitayatorn

Journal Name: Medicinal Chemistry

Volume 9 , Issue 3 , 2013

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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).

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

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Article Details

Year: 2013
Published on: 21 February, 2013
Page: [329 - 339]
Pages: 11
DOI: 10.2174/1573406411309030003
Price: $65

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