A new series of coumarin-yl-chalcone derivatives () had been designed and synthesized through different reactions such as aromatic addition, cyclization and Claisen-Schmidt reactions in good yields (54-78%). 5-acetyl-4-(2-hydroxyphenyl) -6-methyl-3, 4-dihydropyrimidin-2(1H) -one has been synthesized by multi-component one pot reaction of salicylaldehyde, methyl acetoacetate and urea, which was further reacted with malonic acid employing ZnCl catalyst to yield 5-acetyl-4-(4-hydroxy-2-oxo-2-chromen-8-yl) -6-methyl-3, 4-dihydropyrimidin-2(1) -one The title compounds ( were synthesised by reacting 5-acetyl-4-(4-hydroxy-2-oxo-2-chromen-8-yl) -6-methyl-3, 4-dihydropyrimidin-2(1)-one () with different aromatic aldehydes in the presence of potassium hydroxide. studies, a preliminary screening method for predicting the anti-cancer activity was performed for the synthesized compounds ( against Src, Alb tyrosine kinase and homology model protein (PDB ID: 4csv). The derivatives and showed moderate binding energies. The cytotoxic activity was evaluated for the compounds and by using human cancer cell-line morphology and MTT assay against three human cell-lines A549 (Lung), Jurkat (Leukemia) and MCF-7 (Breast). The results indicate that the derivatives and display significant anti-cancer activity, however it was found to be less cytotoxic when compared to the standard used i.e. Imatinib.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7783654PMC
http://dx.doi.org/10.1016/j.sjbs.2020.10.020DOI Listing

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