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

A series of N 1 ,N 3 -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. Compo...

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Bibliographic Details
Published in:Journal of enzyme inhibition and medicinal chemistry 2019-01, Vol.34 (1), p.1247-1258
Main Authors: Kassem, Asmaa F., Moustafa, Gaber O., Nossier, Eman S., Khalaf, Hemat S., Mounier, Marwa M., Al-Yousef, Suliman A., Mahmoud, Sabry Y.
Format: Article
Language:English
Subjects:
amino acids
anticancer activity
Isophthalamide
molecular docking
peptides
Research Paper
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Summary:A series of N 1 ,N 3 -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.
ISSN:1475-6366
1475-6374
DOI:10.1080/14756366.2019.1613390