Potential cytotoxic and selective effect of new benzo[b]xanthenes against oral squamous cell carcinoma.
FUTURE MEDICINAL CHEMISTRY(2018)
摘要
The current work shows a new synthetic methodology to obtain 21 naphthoquinones that have been evaluated against oral cavity cancer. The compounds were obtained by a three-component reaction involving lawsone, dimedone and aromatic aldehydes catalyzed by lithium chloride undermicrowave irradiation to produce families of 1,4-and 1,2-naphthoquinones. Results: A clonogenic assay was performed on SCC9 cell line cultures with all compounds, revealing five very active compounds. In the 3,4,5-dimethylthiazol2,5-diphenyltetrazolium bromide cell viability assay using three different cell lines (SCC9, SCC4 and SCC25), 8c had an average IC50 of approximately 1.45 mu M capable of reducing tumor cell viability, approximately 90-times higher than carboplatin. Conclusion: Therefore, the xanthene-naphthoquinone derivatives show promising bioactivity for oral cavity cancer treatment.
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关键词
clonogenic assay,cytotoxicity,hemolytic activity,Knoevenagel condensation,lapachones,lawsone,multicomponent reactions
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