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

Mostafa M. Ghorab, Mansour S. Alsaid, Marwa G. El-Gazzar, Maureen Higgins, Albena T. Dinkova-Kostova, Abdelaaty A. Shahat

Research output: Contribution to journal › Article

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, 1H-NMR, 13C-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 (US)
Pages (from-to)1-6
Number of pages6
JournalJournal of Enzyme Inhibition and Medicinal Chemistry
DOIs
StateAccepted/In press - Jan 20 2016

Keywords

  • 4-aminoquinazoline
  • cytoprotective
  • NAD(P)H
  • synthesis

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology

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    Ghorab, M. M., Alsaid, M. S., El-Gazzar, M. G., Higgins, M., Dinkova-Kostova, A. T., & Shahat, A. A. (Accepted/In press). NAD(P)H: quinone oxidoreductase 1 inducer activity of novel 4-aminoquinazoline derivatives. Journal of Enzyme Inhibition and Medicinal Chemistry, 1-6. https://doi.org/10.3109/14756366.2015.1135913