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.
Original language | English |
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Pages (from-to) | 1369-1374 |
Number of pages | 7 |
Journal | Journal of Enzyme Inhibition and Medicinal Chemistry |
Volume | 31 |
Issue number | 6 |
Early online date | 21 Jan 2016 |
DOIs | |
Publication status | Published - 2016 |
Keywords
- anilinoquinazoline
- molecular modeling
- Keap1/Nrf2
- cytoprotection
- NQO1 induction