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 journalArticle

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

Fingerprint

NAD
Oxidoreductases
Enzymes
4-aminoquinazoline
Proton Magnetic Resonance Spectroscopy
Carbon-13 Magnetic Resonance Spectroscopy
benzoquinone

Keywords

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

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology

Cite this

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

NAD(P)H : quinone oxidoreductase 1 inducer activity of novel 4-aminoquinazoline derivatives. / Ghorab, Mostafa M.; Alsaid, Mansour S.; El-Gazzar, Marwa G.; Higgins, Maureen; Dinkova-Kostova, Albena T.; Shahat, Abdelaaty A.

In: Journal of Enzyme Inhibition and Medicinal Chemistry, 20.01.2016, p. 1-6.

Research output: Contribution to journalArticle

Ghorab, Mostafa M. ; Alsaid, Mansour S. ; El-Gazzar, Marwa G. ; Higgins, Maureen ; Dinkova-Kostova, Albena T. ; Shahat, Abdelaaty A. / NAD(P)H : quinone oxidoreductase 1 inducer activity of novel 4-aminoquinazoline derivatives. In: Journal of Enzyme Inhibition and Medicinal Chemistry. 2016 ; pp. 1-6.
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