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

Autor: Bazanov DR; Department of Chemistry, M. V. Lomonosov Moscow State University, 119992 Moscow, Russia., Pervushin NV; Department of Medicine, M. V. Lomonosov Moscow State University, 119991 Moscow, Russia., Savin EV; Department of Medicine, M. V. Lomonosov Moscow State University, 119991 Moscow, Russia., Tsymliakov MD; Department of Chemistry, M. V. Lomonosov Moscow State University, 119992 Moscow, Russia., Maksutova AI; Department of Chemistry, M. V. Lomonosov Moscow State University, 119992 Moscow, Russia., Savitskaya VY; Department of Chemistry, M. V. Lomonosov Moscow State University, 119992 Moscow, Russia., Sosonyuk SE; Department of Chemistry, M. V. Lomonosov Moscow State University, 119992 Moscow, Russia., Gracheva YA; Department of Chemistry, M. V. Lomonosov Moscow State University, 119992 Moscow, Russia., Seliverstov MY; Department of Chemistry, M. V. Lomonosov Moscow State University, 119992 Moscow, Russia., Lozinskaya NA; Department of Chemistry, M. V. Lomonosov Moscow State University, 119992 Moscow, Russia., Kopeina GS; Department of Medicine, M. V. Lomonosov Moscow State University, 119991 Moscow, Russia.
Jazyk: angličtina
Zdroj: Pharmaceuticals (Basel, Switzerland) [Pharmaceuticals (Basel)] 2022 Apr 02; Vol. 15 (4). Date of Electronic Publication: 2022 Apr 02.
DOI: 10.3390/ph15040444
Abstrakt: 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: MEDLINE
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