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- Title
Synthetic Design and Biological Evaluation of New p53-MDM2 Interaction Inhibitors Based on Imidazoline Core.
- Authors
Bazanov, Daniil R.; Pervushin, Nikolay V.; Savin, Egor V.; Tsymliakov, Michael D.; Maksutova, Anita I.; Savitskaya, Victoria Yu.; Sosonyuk, Sergey E.; Gracheva, Yulia A.; Seliverstov, Michael Yu.; Lozinskaya, Natalia A.; Kopeina, Gelina S.
- 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.
- Subjects
IMIDAZOLINES; P53 protein; PROTEIN-protein interactions; CELL lines; ANTINEOPLASTIC agents; CANCER cells
- Publication
Pharmaceuticals (14248247), 2022, Vol 15, Issue 4, pN.PAG
- ISSN
1424-8247
- Publication type
Article
- DOI
10.3390/ph15040444