A new series of coumarin-yl-chalcone derivatives (3a-m) 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 (1) has been synthesized by multi-component one pot reaction of salicylaldehyde, methyl acetoacetate and urea, which was further reacted with malonic acid employing ZnCl₂ catalyst to yield 5-acetyl-4-(4-hydroxy-2-oxo-2H-chromen-8-yl) -6-methyl-3, 4-dihydropyrimidin-2(1H) -one (2). The title compounds (3a-m) were synthesised by reacting 5-acetyl-4-(4-hydroxy-2-oxo-2H-chromen-8-yl) -6-methyl-3, 4-dihydropyrimidin-2(1H)-one (2) with different aromatic aldehydes in the presence of potassium hydroxide. In silico studies, a preliminary screening method for predicting the anti-cancer activity was performed for the synthesized compounds (3a-m) against Src, Alb tyrosine kinase and homology model protein (PDB ID: 4csv). The derivatives 3h and 3m showed moderate binding energies. The in vitro cytotoxic activity was evaluated for the compounds 3h and 3m 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 3h and 3m display significant anti-cancer activity, however it was found to be less cytotoxic when compared to the standard used i.e. Imatinib.

通过芳香加成、环化和克莱森-施密特反应等不同反应，设计并合成了一系列新的香豆素-基查尔酮衍生物 ( 3a-m )，收率良好 (54-78%)。5-乙酰基-4-(2-羟基苯基) -6-methyl-3, 4-dihydropyrimidin-2(1H) -one (1)采用水杨醛、乙酰乙酸甲酯和尿素的多组分一锅法反应合成。使用 ZnCl ₂催化剂进一步与丙二酸反应生成5-acetyl-4-(4-hydroxy-2-oxo-2 H -chromen-8-yl) -6-methyl-3, 4-dihydropyrimidin-2(1 H )-一(2)。标题化合物 ( 3a-m)由 5-乙酰基-4-(4-羟基-2-氧代-2 H ) 反应合成-chromen-8-yl) -6-methyl-3, 4-dihydropyrimidin-2(1 H )-one ( 2 ) 在氢氧化钾存在下与不同的芳香醛。在计算机研究中，对合成的化合物 ( 3a-m)针对 Src、Alb 酪氨酸激酶和同源模型蛋白 (PDB ID: 4csv)进行了预测抗癌活性的初步筛选方法。衍生物3h和3m显示出中等的结合能。评价化合物3h和3m的体外细胞毒活性通过使用人类癌细胞系形态学和针对三种人类细胞系 A549 (Lung)、Jurkat (Leukemia) 和 MCF-7 (Breast) 的 MTT 测定。结果表明，衍生物3h和3m显示出显着的抗癌活性，但与使用的标准品（即伊马替尼）相比，发现其细胞毒性较小。