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

  • Asmaa F. Kassem
  • , Gaber O. Moustafa
  • , Eman S. Nossier
  • , Hemat S. Khalaf
  • , Marwa M. Mounier
  • , Suliman A. Al-Yousef
  • , Sabry Y. Mahmoud

Research output: Contribution to journalArticlepeer-review

38 Scopus citations

Abstract

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.

Original languageEnglish
Pages (from-to)1247-1258
Number of pages12
JournalJournal of Enzyme Inhibition and Medicinal Chemistry
Volume34
Issue number1
DOIs
StatePublished - 1 Jan 2019
Externally publishedYes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

  1. SDG 3 - Good Health and Well-being
    SDG 3 Good Health and Well-being

Keywords

  • amino acids
  • anticancer activity
  • Isophthalamide
  • molecular docking
  • peptides

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