| Title |
NAD(P)H:quinone oxidoreductase 1 inducer activity of some novel anilinoquinazoline derivatives
|
|---|---|
| Published in |
Drug Design, Development and Therapy, August 2016
|
| DOI | 10.2147/dddt.s105423 |
| Pubmed ID | |
| Authors |
Mostafa M Ghorab, Mansour S Alsaid, Maureen Higgins, Albena T Dinkova-Kostova, Abdelaaty A Shahat, Nehal H Elghazawy, Reem K Arafa |
| Abstract |
The Kelch-like ECH-associated protein 1 (Keap1)/nuclear factor erythroid 2-related factor 2 (Nrf2)/antioxidant response elements pathway enables cells to survive oxidative stress conditions through regulating the expression of cytoprotective enzymes such as quinone oxidoreductase 1 (NQO1). This work presents the design and synthesis of novel anilinoquinazoline derivatives (2-16a) and evaluation of their NQO1 inducer activity in murine cells. Molecular docking of the new compounds was performed to assess their ability to inhibit Keap1-Nrf2 protein-protein interaction through occupying the Keap1-Nrf2-binding domain, which leads to Nrf2 accumulation and enhanced gene expression of NQO1. Docking results showed that all compounds can potentially interact with Keap1; however, 1,5-dimethyl-2-phenyl-4-(2-phenylquinazolin-4-ylamino)-1,2-dihydropyrazol-3-one (9), the most potent inducer, showed the largest number of interactions with key amino acids in the binding pocket (Arg483, Tyr525, and Phe478) compared to the native ligand or any other compound in this series. |
X Demographics
The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Practitioners (doctors, other healthcare professionals) | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 19 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 19 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Professor | 3 | 16% |
| Other | 2 | 11% |
| Student > Master | 2 | 11% |
| Student > Ph. D. Student | 2 | 11% |
| Student > Doctoral Student | 1 | 5% |
| Other | 1 | 5% |
| Unknown | 8 | 42% |
| Readers by discipline | Count | As % |
|---|---|---|
| Arts and Humanities | 1 | 5% |
| Pharmacology, Toxicology and Pharmaceutical Science | 1 | 5% |
| Biochemistry, Genetics and Molecular Biology | 1 | 5% |
| Agricultural and Biological Sciences | 1 | 5% |
| Sports and Recreations | 1 | 5% |
| Other | 2 | 11% |
| Unknown | 12 | 63% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 09 August 2016.
All research outputs
#20,674,485
of 25,394,764 outputs
Outputs from Drug Design, Development and Therapy
#1,440
of 2,270 outputs
Outputs of similar age
#299,585
of 381,115 outputs
Outputs of similar age from Drug Design, Development and Therapy
#42
of 76 outputs
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