A new series of N-(4-(1-Phenyl-5-aryl-4,5-dihydro-1H-pyrazol-3-yl)phenyl)-4-substitutedbenzamide derivatives were designed and synthesized from new chalcone derivatives. All newly synthesized compounds were determined by using IR, ¹H-NMR, ¹³C-NMR spectroscopic methods, elemental analysis and evaluated for their in vitro antiproliferative activities on HeLa, MCF-7, MKN-45 cancer cell lines and NIH-3T3 cell line using MTT assay. Expression of Bax and Bcl-2 proteins was detected by Western-blot analysis and caspase-3 enzyme activity was measured. Notably, compounds 1f and 2f showed a significant cytotoxic effect in all three cancer cells and did not display cytotoxicity on NIH-3T3 normal cells. (IC₅₀ = 26.66 ± 2.73 μM on HeLa, IC₅₀ = 9.41 ± 2.19 μM on MCF-7, IC₅₀ = 5.17 ± 3.54 μM on MKN-45 for 1f. IC₅₀ = 17.96 ± 3.34 μM on HeLa, IC₅₀ = 0.69 ± 0.13 μM on MCF-7, IC₅₀ = 0.88 ± 0.16 μM on MKN-45 for 2f.) Moreover, 1f and 2f upregulated protein expression level of Bax and downregulated protein expression level of Bcl-2 in cells. Similarly, caspase-3 activity was increased in cells via 1f and 2f. It can be concluded that 1f and 2f activated apoptosis by inducing mitochondrial apoptotic proteins in HeLa, MCF-7, MKN-45. This could be potentially new anti-cancer derivatives and used to contribute to new therapeutic development.

设计并合成了新的查尔酮衍生物，合成了一系列新的N-（4-（1-苯基-5-芳基-4,5-二氢-1H-吡唑-3-基）苯基）-4-取代的苯甲酰胺衍生物。使用IR，¹ H-NMR，¹³ C-NMR光谱法，元素分析确定所有新合成的化合物，并评估其对HeLa，MCF-7，MKN-45癌细胞系和NIH-3T3细胞的体外抗增殖活性使用MTT分析的线。通过蛋白质印迹分析检测Bax和Bcl-2蛋白的表达，并测量caspase-3酶活性。值得注意的是，化合物1f和2f在所有三种癌细胞中均显示出显着的细胞毒性作用，对NIH-3T3正常细胞未显示出细胞毒性。（IC ₅₀  = 26.66±2.73μM对HeLa，IC ₅₀  = 9.41±2.19μM对MCF-7，IC ₅₀  = 5.17±3.54μM上MKN-45为1F。IC ₅₀  = 17.96±3.34μM对HeLa，IC ₅₀  = 对于2f，在MCF-7上为0.69±0.13μM，在MKN-45上，IC ₅₀ = 0.88± 0.16μM。）此外，1f和2f上调了细胞中Bax的蛋白表达水平，并下调了Bcl-2的蛋白表达水平。同样，caspase-3活性通过1f和2f在细胞中增加。可以得出结论，1f和2f通过诱导HeLa，MCF-7，MKN-45中的线粒体凋亡蛋白来激活细胞凋亡。这可能是潜在的新抗癌衍生物，并有助于新的治疗方法的发展。