Abstract

N-Substituted imides, isoindoline-1,3-dione derivatives, were synthesized, characterized, and investigated against blood cancer using K562 and Raji cell lines. Cytotoxicity assay was performed to determine the influence of phthalimide derivatives on the survival of the cancer cells. In addition, flow-cytometry with annexin-V-conjugated with fluorescein isothiocyanate (FITC) and propidium iodide (PI) stains were used to investigate the type of cell death induced by our phthalimide derivatives. 2-(4-(2-Bromoacetyl)phenyl)isoindoline-1,3-dione showed the most inhibitory effect on the viability of the cancer cells (CC₅₀ = 0.26 µg/mL for Raji cells and 3.81 µg/mL for K562 cells). As a result, 2-(4-(2-bromoacetyl)phenyl)isoindoline-1,3-dione was selected for further investigations to determine the type of cellular death against Raji cells. The analysis found that this compound induced apoptosis and necrosis in Raji cells. Our findings provide a basis for a further study to investigate the impact of additional alkylating imides on the survival of blood cancer cells, particularly against Raji cells.

中文翻译：

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新型异吲哚啉-1,3-二酮衍生物作为抗癌剂的合成与评价

摘要

使用K562和Raji细胞系合成，表征N-取代的酰亚胺，即异吲哚啉-1,3-二酮衍生物，并研究抗血癌的方法。进行细胞毒性测定以确定邻苯二甲酰亚胺衍生物对癌细胞存活的影响。此外，流式细胞术结合膜联蛋白-V与异硫氰酸荧光素（FITC）和碘化丙啶（PI）染色共轭，用于研究由我们的邻苯二甲酰亚胺衍生物诱导的细胞死亡类型。2-（4-（2-溴乙酰基）苯基）异吲哚啉-1,3-二酮显示出对癌细胞活力的最大抑制作用（CC ₅₀对于Raji细胞= 0.26 µg / mL，对于K562细胞= 3.81 µg / mL）。结果，选择2-（4-（2-溴乙酰基）苯基）异吲哚啉-1,3-二酮用于进一步研究以确定针对Raji细胞的细胞死亡类型。分析发现该化合物诱导Raji细胞凋亡和坏死。我们的发现为进一步研究其他烷基化酰亚胺对血液癌细胞（尤其是针对Raji细胞）存活的影响提供了基础。