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. (1st January 2019)

• Record Type: Journal Article
• Authors: Kassem, Asmaa F.; Moustafa, Gaber O.; Nossier, Eman S.; Khalaf, Hemat S.; Mounier, Marwa M.; Al-Yousef, Suliman A.; Mahmoud, Sabry Y.
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 34:Number 1(2019)
• Page Start: 1247
• Page End: 1258
• Publication Date: 2019-01-01
• Subjects: Isophthalamide -- amino acids -- peptides -- anticancer activity -- molecular docking; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.1080/14756366.2019.1613390
• Languages: English
• ISSNs: 1475-6366

Abstract

Abstract: 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.