Abstract：
A series of spirocyclopropyl oxindoles with benzimidazole substitutions was synthesized and tested for their cytotoxicity against selected human cancer cells. Most of the molecules exhibited significant antiproliferative activity with compound 12 p being the most potent. It exhibited significant cytotoxicity against MCF-7 breast cancer cells (IC50 value 3.14±0.50 μM), evidenced by the decrease in viable cells and increased apoptotic features during phase contrast microscopy, such as AO/EB, DAPI and DCFDA staining studies. Compound 12 p also inhibited cell migration in wound healing assay. Anticancer potential of 12 p was proved by the inhibition of tubulin polymerization with IC50 of 5.64±0.15 μM. These results imply the potential of benzimidazole substituted spirocyclopropyl oxindoles, notably 12 p, as cytotoxic agent for the treatment of breast cancer.
摘要：
合成了一系列具有苯并咪唑取代的螺环丙基羟吲哚，并测试了它们对选定的人癌细胞的细胞毒性。大多数分子表现出显著的抗增殖活性,其中化合物12p是最有效的。它对MCF-7乳腺癌细胞表现出显著的细胞毒性（IC50值3.14±0.50μM），在相差显微镜期间，活细胞的减少和凋亡特征的增加证明，如AO/EB，DAPI和DCFDA染色研究。化合物12p还抑制伤口愈合测定中的细胞迁移。通过抑制微管蛋白聚合，IC50为5.64±0.15μM，证明了12p的抗癌潜力。这些结果暗示了苯并咪唑取代的螺环丙基羟吲哚的潜力，特别是12页，作为治疗乳腺癌的细胞毒性剂。
