In vitro anticancer potentiality and molecular modelling study of novel amino acid derivatives based on N1,N3-bis-(1-hydrazinyl-1-oxopropan-2-yl) isophthalamide

Journal of Enzyme Inhibition and Medicinal Chemistry

Eman S. Nossier¹  Hemat S. Khalaf²  Sabry Y. Mahmoud³  Asmaa F. Kassem⁴  Marwa M. Mounier⁴  Gaber O. Moustafa⁴  Suliman A. Al-Yousef⁵ 

[1] Al-Azhar University;College of Science and Arts, Jouf University;College of Science, University of Hafr Al Batin;National Research Centre;University of Hafr Al Batin;

关键词: isophthalamide;    amino acids;    peptides;    anticancer activity;    molecular docking;   

DOI  :  10.1080/14756366.2019.1613390

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown