合成了八种新型查尔酮，并通过不同的光谱工具证实了它们的结构。所有制备的化合物均针对几种癌细胞系进行了 SRB 细胞毒性筛选。化合物 5c 对 MCF7 和 HEP2 细胞发挥了最有希望的作用，IC50 值分别为 9.5 和 12 µg/mL。实时PCR证明化合物5c对抗原kiel 67 (KI-67)、Survivin、Interleukin-1beta (IL-1B)、Interleukin-6 (IL-6)、Cyclooxygenase-2 (COX)表达水平的抑制作用-2) 和蛋白激酶 B (AKT1) 基因。细胞周期的流式细胞术分析表明，化合物5c分别使MCF7和HEP2处理的细胞的细胞周期停止在G0/G1和G2/M期。 ELISA 检测显示 Caspase 8、Caspase 9、P53、BAX 和谷胱甘肽 (GSH) 极度激活，基质金属蛋白酶 2 (MMP2)、基质金属蛋白酶 9 (MMP9)、BCL2、丙二醛 (MDA) 和 IL-6 失活在5c处理的MCF7和HEP2细胞中。伤口愈合显示，48 小时后，与未处理的细胞相比，查耳酮 5c 降低了闭合擦伤伤口的能力，并减少了迁移的 MCF7 和 HEP2 细胞的数量。针对 P53 癌症突变体 Y220C 和 Bcl2 的理论分子模型显示结合能分别为 -22.8 和 -24.2 Kcal/摩尔，这证实了我们的 ELISA 结果。© 2024。作者。

Eight Novel chalcones were synthesized and their structures were confirmed by different spectral tools. All the prepared compounds were subjected to SRB cytotoxic screening against several cancer cell lines. Compound 5c exerted the most promising effect against MCF7 and HEP2 cells with IC50 values of 9.5 and 12 µg/mL, respectively. Real-time PCR demonstrated the inhibitory effect of compound 5c on the expression level of Antigen kiel 67 (KI-67), Survivin, Interleukin-1beta (IL-1B), Interleukin-6 (IL-6), Cyclooxygenase-2 (COX-2) and Protein kinase B (AKT1) genes. Flow-cytometric analysis of the cell cycle indicated that compound 5c stopped the cell cycle at the G0/G1 and G2/M phases in MCF7 and HEP2 treated cells, respectively. ELISA assay showed that Caspase 8, Caspase 9, P53, BAX, and Glutathione (GSH) were extremely activated and Matrix metalloproteinase 2 (MMP2), Matrix metalloproteinase 9 (MMP9), BCL2, Malondialdehyde (MDA), and IL-6 were deactivated in 5c treated MCF7 and HEP2 cells. Wound healing revealed that chalcone 5c reduced the ability to close the scrape wound and decreased the number of migrating MCF7 and HEP2 cells compared to the untreated cells after 48 h. Theoretical molecular modeling against P53 cancer mutant Y220C and Bcl2 showed binding energies of -22.8 and -24.2 Kcal/mole, respectively, which confirmed our ELISA results.© 2024. The Author(s).