Methoxyphenyl Imidazolines as Potential Activators of p53
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 the p53-mdm2 interaction have been proposed. The two-step synthesis of the imidazoline core with subsequent modifications for...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2022-11-01
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| Series: | Medical Sciences Forum |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2673-9992/14/1/100 |
| Summary: | 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 the 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 caused the accumulation of p53 protein levels more than seven times than in comparison with the control. The accumulation of proapoptotic proteins such as p21 and PUMA has also been investigated, and the mechanism of cell death has been shown. |
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| ISSN: | 2673-9992 |