Synthetic Design and Biological Evaluation of New p53-MDM2 Interaction Inhibitors Based on Imidazoline Core

Autor:	Daniil R. Bazanov, Nikolay V. Pervushin, Egor V. Savin, Michael D. Tsymliakov, Anita I. Maksutova, Victoria Yu. Savitskaya, Sergey E. Sosonyuk, Yulia A. Gracheva, Michael Yu. Seliverstov, Natalia A. Lozinskaya, Gelina S. Kopeina
Jazyk:	angličtina
Rok vydání:	2022
Předmět:	nutlins cis-imidazolines p53-MDM2 inhibitors anti-cancer Medicine Pharmacy and materia medica RS1-441
Zdroj:	Pharmaceuticals, Vol 15, Iss 4, p 444 (2022)
Druh dokumentu:	article
ISSN:	1424-8247
DOI:	10.3390/ph15040444
Popis:	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.
Databáze:	Directory of Open Access Journals
Externí odkaz:	https://doaj.org/article/86381fec34274d868b2c6af77b718cf2 Zobrazit plný text záznamu View record in DOAJ Plný text ve formátu PDF Plný text ve formátu HTML
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