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新型基于,-双-(1-肼基-1-氧代-2-丙基)异酞酰亚胺氨基酸衍生物的抗癌潜力及分子建模研究。

anticancer potentiality and molecular modelling study of novel amino acid derivatives based on ,-bis-(1-hydrazinyl-1-oxopropan-2-yl) isophthalamide.

机构信息

a Department of Chemistry of Natural and Microbial Products, Pharmaceutical and Drug Industries Research Division , National Research Centre , Giza , Egypt.

b Department of Peptide Chemistry, Chemical Industries Research Division , National Research Centre , Cairo , Egypt.

出版信息

J Enzyme Inhib Med Chem. 2019 Dec;34(1):1247-1258. doi: 10.1080/14756366.2019.1613390.

Abstract

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

摘要

制备了一系列基于 - 的衍生物,并通过不同的光谱工具确证了它们的结构。通过 MTT 法测定了新型化合物 - 对结肠、肺和乳腺肿瘤细胞系的细胞毒性潜力。化合物 - 表现出最显著的特异性抗癌活性,对正常细胞系具有安全反应。还检查了 酶测定和几种凋亡参数,以阐明化合物 - 的作用模式。还进行了分子对接研究,以深入了解其结构特征。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4b0/6691786/f0be8532b08d/IENZ_A_1613390_F0001_C.jpg

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