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Synthesis and Biological Evaluation of Some New 3,4-Disubstituted Coumarin Derivatives as Anticancer Agents

Eman Mossad Mahmoud Radwan, El-Sherbiny Hamdy El-Sayed Yuossif,Mohamed Abd El-Moneim, Mahmoud Mohamed,Amal Mahmoud Youssef Moustafa

INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY(2021)

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Abstract
A new series of 3,4-disubstitutued coumarin derivatives have been synthesized by the reaction of ethyl coumarin-3-carboxylate with pyrazole-3,5-dione and condensation of ethyl 7-hydroxycoumarin-3-carboxylate with 4,6-dibromo-3-amino phenol. Acylation with acetic anhydride and condensation of coumarin derivatives with 2-hydroxybenzaldehyde yielded the corresponding acetyl derivatives and 4-substituted pyrazole derivatives. The structure of the synthesized compounds was elucidated using spectral and elemental analysis. All the prepared derivatives were evaluated for their cytotoxicity against human breast carcinoma cell line (MCF-7). Compound VI has shown the least IC50 values in dimethylthiazol-diphenyltetrazolium bromide colorimetric assay compared with that of the standard marketed drug, staurosporine drug.
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Key words
Apoptosis,Breast cancer,Cell cycle,Coumarin,Pyrazole
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