Events 8th International Electronic Conference on Medicinal Chemistry

Event submissions

Published

10.3390/ECMC2022-13494

This submission belongs to the session S3. General of the event 8th International Electronic Conference on Medicinal Chemistry

Published date

07 Nov, 2022

Academic Editor

Amélia Pilar Rauter

Citation

Daniil Bazanov, Nikolay Pervushin, Natalia Lozinskaya, Gelina Kopeina, Methoxyphenylimidazolines as potential activators of p53, in Proceedings of 8th International Electronic Conference on Medicinal Chemistry, 1 November–30 November 2022, MDPI: Basel, Switzerland, doi: 10.3390/ECMC2022-13494

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Methoxyphenylimidazolines as potential activators of p53

Daniil Bazanov ¹

Nikolay Pervushin ²

Natalia Lozinskaya ³

Gelina Kopeina ²

1. Department of Chemistry, M. V. Lomonosov Moscow State University, Russia

2. Department of Medicine, M. V. Lomonosov Moscow State University

3. Department of Chemistry, M. V. Lomonosov Moscow State University

Abstract

The use of p53-MDM2/X inhibitors is a prospective strategy in anti-cancer therapy for tumors with wild type p53 protein. In our study new low molecular weight inhibitors of p53-mdm2 interaction have been proposed. The two-step synthesis of the imidazoline core with subsequent modifications for the nitrogen atom was carried out. New molecules cause the accumulation of p53 protein levels more than 7 times in comparison with the control. The accumulation of proapoptotic proteins such as p21, PUMA has also been investigated, and the mechanism of cell death has been shown.

Keywords

p53

nutlin

mdm2

mdmX

Poster

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