Ibrahim Hany S, Abou-Seri Sahar M, Ismail Nasser S M, Elaasser Mahmoud M, Aly Mohamed H, Abdel-Aziz Hatem A
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Egyptian Russian University, Badr City, Cairo 11829, Egypt.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo 11562, Egypt.
Eur J Med Chem. 2016 Jan 27;108:415-422. doi: 10.1016/j.ejmech.2015.11.047. Epub 2015 Dec 2.
Many bis-isatins and isatins with hydrazide extension were reported to have a potential anti-proliferative effects against different cancer cell lines and cancer targets. In this study, four series of bis-isatins with hydrazide linkers were synthesized. These compounds were investigated for their antitumor activity by assessing their cytotoxic potency against HepG2, MCF-7 and HCT-116 cancer cell lines. Compound 21c possessed significant cytotoxic activity against MCF-7 (IC50 = 1.84 μM) and HCT-116 (IC50 = 3.31 μM) that surpasses the activity of doxorubicin against both cell lines (MCF-7; IC50 = 2.57 μM and HCT-116; IC50 = 3.70 μM). Cell cycle analysis and annexin V-FITC staining of MCF-7 cells treated with 21c suggested that the cytotoxic effect of the compound could be attributed to its pro-apoptotic activity.
据报道，许多双异吲哚酮和带有酰肼延伸基团的异吲哚酮对不同癌细胞系和癌症靶点具有潜在的抗增殖作用。在本研究中，合成了四个系列带有酰肼连接基团的双异吲哚酮。通过评估这些化合物对HepG2、MCF-7和HCT-116癌细胞系的细胞毒性效力，对其抗肿瘤活性进行了研究。化合物21c对MCF-7（IC50 = 1.84 μM）和HCT-116（IC50 = 3.31 μM）具有显著的细胞毒性活性，超过了阿霉素对这两种细胞系的活性（MCF-7；IC50 = 2.57 μM和HCT-116；IC50 = 3.70 μM）。对用21c处理的MCF-7细胞进行细胞周期分析和膜联蛋白V-FITC染色表明，该化合物的细胞毒性作用可能归因于其促凋亡活性。
