A series of new (Z)-3-(3′-methoxy-4′-(2-amino-2-oxoethoxy)benzylidene)indolin-2-one derivatives has been synthesized and evaluated for their cytotoxic activity against selected human cancer cell lines of prostate (PC-3 and DU-145), breast (BT-549 and MDA-MB-231) and non-tumorigenic prostate epithelial cells (RWPE-1). Among the tested, one of the compounds 4p exhibited potent cytotoxicity selectively on prostate cancer cell lines (PC-3 and DU-145; IC₅₀: 1.89 ± 0.6 and 1.94 ± 0.2 μM, respectively). Further experiments were conducted with 4p on PC-3 cancer cells to study the mechanisms of growth inhibition and apoptosis inducing effect. Treatment of PC-3 cells with test compound 4p resulted in inhibition of cell migration through disorganization of F-actin protein. The flow-cytometry analysis results showed that the compound arrested PC-3 cancer cells in the G2/M phase of cell cycle in a dose dependent manner. Hoechst staining and annexin–V binding assay revealed that the compound 4p inhibited tumor cell proliferation through induction of apoptosis. Western blot studies demonstrated that the compound 4p treatment led to activation of caspase-3, increased expression of pro-apoptotic Bax and significantly decreased expression of anti-apoptotic Bcl-2 in human prostate cancer PC-3 cells. In addition, the mitochondrial membrane potential (ΔΨm) was also affected and the levels of intracellular Ca²⁺ were raised.

合成了一系列新的（Z）-3-（3'-甲氧基-4'-（2-氨基-2-氧代乙氧基）亚苄基）吲哚-2-酮衍生物，并评估了其对所选人类癌细胞的细胞毒性活性前列腺（PC-3和DU-145），乳腺（BT-549和MDA-MB-231）和非致瘤性前列腺上皮细胞（RWPE-1）。在测试的化合物中，化合物4p之一对前列腺癌细胞系选择性地表现出有效的细胞毒性（PC-3和DU-145； IC ₅₀：分别为1.89±0.6和1.94±0.2μM）。以4p对PC-3癌细胞进行了进一步的实验，以研究其生长抑制和凋亡诱导作用的机制。用测试化合物4p处理PC-3细胞导致细胞迁移通过F-肌动蛋白蛋白的紊乱而受到抑制。流式细胞仪分析结果表明该化合物以剂量依赖的方式将PC-3癌细胞阻滞在细胞周期的G2 / M期。Hoechst染色和膜联蛋白-V结合试验表明，化合物4p通过诱导凋亡来抑制肿瘤细胞的增殖。蛋白质印迹研究表明，化合物4p处理可导致人前列腺癌PC-3细胞中caspase-3活化，促凋亡Bax表达增加以及抗凋亡Bcl-2表达明显降低。另外，线粒体膜电位（ΔΨm）也受到影响，细胞内Ca ^2+的水平升高。