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

J Enzyme Inhib Med Chem. 2016 Dec;31(6):1369-74. doi: 10.3109/14756366.2015.1135913. Epub 2016 Jan 21.

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.

Keywords: 4-aminoquinazoline; NAD(P)H; cytoprotective; synthesis.

MeSH terms

  • Animals
  • Cell Line
  • Enzyme Induction / drug effects*
  • Mice
  • NAD(P)H Dehydrogenase (Quinone) / biosynthesis*
  • Quinazolines / pharmacology
  • Spectrum Analysis / methods

Substances

  • 4-aminoquinazoline
  • Quinazolines
  • NAD(P)H Dehydrogenase (Quinone)
  • Nqo1 protein, mouse