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Synthetic Design and Biological Evaluation of New p53-MDM2 Interaction Inhibitors Based on Imidazoline Core.
- Source :
-
Pharmaceuticals (Basel, Switzerland) [Pharmaceuticals (Basel)] 2022 Apr 02; Vol. 15 (4). Date of Electronic Publication: 2022 Apr 02. - Publication Year :
- 2022
-
Abstract
- The use of p53-MDM2 inhibitors is a prospective strategy in anti-cancer therapy for tumors expressing wild type p53 protein. In this study, we have applied a simple approach of two-step synthesis of imidazoline-based alkoxyaryl compounds, which are able to efficiently inhibit p53-MDM2 protein-protein interactions, promote accumulation of p53 and p53-inducible proteins in various cancer cell lines. Compounds 2l and 2k cause significant upregulation of p53 and p53-inducible proteins in five human cancer cell lines, one of which possesses overexpression of MDM2.
Details
- Language :
- English
- ISSN :
- 1424-8247
- Volume :
- 15
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Pharmaceuticals (Basel, Switzerland)
- Publication Type :
- Academic Journal
- Accession number :
- 35455441
- Full Text :
- https://doi.org/10.3390/ph15040444