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.
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Methoxyphenylimidazolines as potential activators of p53
Published: 07 November 2022 by MDPI in 8th International Electronic Conference on Medicinal Chemistry session General
Keywords: p53, nutlin, mdm2, mdmX