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

Sabry Y. Mahmoud¹  Asmaa F. Kassem²  Hemat S. Khalaf³  Suliman A. Al-Yousef⁴  Gaber O. Moustafa⁵  Eman S. Nossier⁶  Marwa M. Mounier⁷ 

[1] Department of Biology, College of Science, University of Hafr Al Batin, Hafr Al Batin, Saudi Arabi;Department of Chemistry of Natural and Microbial Products, Pharmaceutical and Drug Industries Research Division, National Research Centre, Giza, Egypt;Department of Chemistry, College of Science and Arts, Jouf University, Al Qurayat, Saudi Arabia;Chemical Industries Research Division, Department of Photochemistry, National Research Centre, Cairo, Egypt;Department of Clinical Laboratory Science, College of Applied Medical Science, University of Hafr Al Batin, Hafr Al Batin, Saudi Arabia;Department of Peptide Chemistry, Chemical Industries Research Division, National Research Centre, Cairo, Egypt;Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt;Pharmaceutical and Drug Industries Research Division, Department of Pharmacognosy, National Research Centre, Giza, Egypt;

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

DOI  :  10.1080/14756366.2019.1613390

来源: publisher

【 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】

CC BY