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

doi:10.3109/14756366.2015.1135913

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

School of Medicine

Research output: Contribution to journal › Article › peer-review

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 language	English (US)
Pages (from-to)	1-6
Number of pages	6
Journal	Journal of Enzyme Inhibition and Medicinal Chemistry
DOIs	https://doi.org/10.3109/14756366.2015.1135913
State	Accepted/In press - Jan 20 2016

Keywords

4-aminoquinazoline
cytoprotective
NAD(P)H
synthesis

ASJC Scopus subject areas

Drug Discovery
Pharmacology

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10.3109/14756366.2015.1135913

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

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.",

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author = "Ghorab, {Mostafa M.} and Alsaid, {Mansour S.} and El-Gazzar, {Marwa G.} and Maureen Higgins and Dinkova-Kostova, {Albena T.} and Shahat, {Abdelaaty A.}",

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doi = "10.3109/14756366.2015.1135913",

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T2 - quinone oxidoreductase 1 inducer activity of novel 4-aminoquinazoline derivatives

AU - Ghorab, Mostafa M.

AU - Alsaid, Mansour S.

AU - El-Gazzar, Marwa G.

AU - Higgins, Maureen

AU - Dinkova-Kostova, Albena T.

AU - Shahat, Abdelaaty A.

PY - 2016/1/20

Y1 - 2016/1/20

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AB - 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.

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KW - cytoprotective

KW - NAD(P)H

KW - synthesis

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

Abstract

Keywords

ASJC Scopus subject areas

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