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 | |
| State | Accepted/In press - Jan 20 2016 |
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Keywords
- 4-aminoquinazoline
- cytoprotective
- NAD(P)H
- synthesis
ASJC Scopus subject areas
- Drug Discovery
- Pharmacology
Cite this
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 journal › Article
}
TY - JOUR
T1 - NAD(P)H
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
N2 - 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.
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.
KW - 4-aminoquinazoline
KW - cytoprotective
KW - NAD(P)H
KW - synthesis
UR - http://www.scopus.com/inward/record.url?scp=84955125298&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84955125298&partnerID=8YFLogxK
U2 - 10.3109/14756366.2015.1135913
DO - 10.3109/14756366.2015.1135913
M3 - Article
C2 - 26796666
AN - SCOPUS:84955125298
SP - 1
EP - 6
JO - Journal of Enzyme Inhibition and Medicinal Chemistry
JF - Journal of Enzyme Inhibition and Medicinal Chemistry
SN - 1475-6366
ER -