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

Authors :
Ghorab MM
Alsaid MS
El-Gazzar MG
Higgins M
Dinkova-Kostova AT
Shahat AA
Source :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2016 Dec; Vol. 31 (6), pp. 1369-74. Date of Electronic Publication: 2016 Jan 21.
Publication Year :
2016

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<br />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.

Details

Language :
English
ISSN :
1475-6374
Volume :
31
Issue :
6
Database :
MEDLINE
Journal :
Journal of enzyme inhibition and medicinal chemistry
Publication Type :
Academic Journal
Accession number :
26796666
Full Text :
https://doi.org/10.3109/14756366.2015.1135913