Abstract

A series of N¹,N³-bis (1-oxopropan-2-yl) isophthalamide-based derivatives 4–16 were prepared and their structures were confirmed by different spectral tools. The cytotoxic potentiality of novel compounds 4–16 was assessed by the MTT assay method on colon, lung and breast tumour cell lines. Compound 5 gave the most significant specificity anticancer activity with safety response on normal cell lines. In vitro enzyme assay and several apoptotic parameters were examined to elucidate the mode of action of compound 5. Molecular docking studies also were simulated to put insight and give better understanding to its structural features.

抽象的

一系列Ñ ¹，N ³ -双（1-氧代丙-2-基）间苯二甲酰胺为基础的衍生物4 - 16制备，并通过不同的光谱工具证实它们的结构。新化合物的细胞毒性潜力4 - 16通过在结肠，肺和乳腺肿瘤细胞系的MTT测定法进行评估。化合物5对正常细胞系具有最显着的特异性抗癌活性，并具有安全性。检查了体外酶测定和一些凋亡参数，以阐明化合物5的作用方式。还对分子对接研究进行了模拟，以提供洞见并更好地理解其结构特征。