NAD(P)H: Quinone oxidoreductase 1 inducer activity of novel 4-aminoquinazoline derivatives

Mostafa M. Ghorab (Lead / Corresponding author), Mansour S. Alsaid, Marwa G. El-Gazzar, Maureen Higgins, Albena T. Dinkova-Kostova, Abdelaaty A. Shahat

    Research output: Contribution to journalArticle

    3 Citations (Scopus)
    149 Downloads (Pure)

    Abstract

    Fourteen novel 4-aminoquinazoline derivatives 2-15 were designed and synthesized. The structure of the newly synthesized compounds was established on the basis of elemental analyses, IR, (1)H-NMR, (13)C-NMR, and mass spectral data. The compounds were evaluated for their potential cytoprotective activity in murine Hepa1c1c7 cells. All of the synthesized compounds showed concentration-dependent ability to induce the cytoprotective enzyme NAD(P)H: quinone oxidoreductase (NQO1) with potencies in the low- to sub-micromolar range. This approach offers an encouraging framework which may lead to the discovery of potent cytoprotective agents.

    Original languageEnglish
    Pages (from-to)1369-1374
    Number of pages7
    JournalJournal of Enzyme Inhibition and Medicinal Chemistry
    Volume31
    Issue number6
    Early online date21 Jan 2016
    DOIs
    Publication statusPublished - 2016

    Keywords

    • anilinoquinazoline
    • molecular modeling
    • Keap1/Nrf2
    • cytoprotection
    • NQO1 induction

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