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: | , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2022-11-01
|
| Series: | Medical Sciences Forum |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2673-9992/14/1/100 |
| _version_ | 1797609801220358144 |
|---|---|
| author | Daniil R. Bazanov Nikolay V. Pervushin Natalia A. Lozinskaya Gelina S. Kopeina |
| author_facet | Daniil R. Bazanov Nikolay V. Pervushin Natalia A. Lozinskaya Gelina S. Kopeina |
| author_sort | Daniil R. Bazanov |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-11T06:06:30Z |
| format | Article |
| id | doaj.art-c1d371c3d969417dbd2c62111727d05a |
| institution | Directory Open Access Journal |
| issn | 2673-9992 |
| language | English |
| last_indexed | 2024-03-11T06:06:30Z |
| publishDate | 2022-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Medical Sciences Forum |
| spelling | doaj.art-c1d371c3d969417dbd2c62111727d05a2023-11-17T12:58:12ZengMDPI AGMedical Sciences Forum2673-99922022-11-0114110010.3390/ECMC2022-13494Methoxyphenyl Imidazolines as Potential Activators of p53Daniil R. Bazanov0Nikolay V. Pervushin1Natalia A. Lozinskaya2Gelina S. Kopeina3Department of Chemistry, M. V. Lomonosov Moscow State University, 119992 Moscow, RussiaDepartment of Medicine, M. V. Lomonosov Moscow State University, 119991 Moscow, RussiaDepartment of Chemistry, M. V. Lomonosov Moscow State University, 119992 Moscow, RussiaDepartment of Medicine, M. V. Lomonosov Moscow State University, 119991 Moscow, RussiaThe 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.https://www.mdpi.com/2673-9992/14/1/100p53nutlinmdm2mdmximidazoline |
| spellingShingle | Daniil R. Bazanov Nikolay V. Pervushin Natalia A. Lozinskaya Gelina S. Kopeina Methoxyphenyl Imidazolines as Potential Activators of p53 Medical Sciences Forum p53 nutlin mdm2 mdmx imidazoline |
| title | Methoxyphenyl Imidazolines as Potential Activators of p53 |
| title_full | Methoxyphenyl Imidazolines as Potential Activators of p53 |
| title_fullStr | Methoxyphenyl Imidazolines as Potential Activators of p53 |
| title_full_unstemmed | Methoxyphenyl Imidazolines as Potential Activators of p53 |
| title_short | Methoxyphenyl Imidazolines as Potential Activators of p53 |
| title_sort | methoxyphenyl imidazolines as potential activators of p53 |
| topic | p53 nutlin mdm2 mdmx imidazoline |
| url | https://www.mdpi.com/2673-9992/14/1/100 |
| work_keys_str_mv | AT daniilrbazanov methoxyphenylimidazolinesaspotentialactivatorsofp53 AT nikolayvpervushin methoxyphenylimidazolinesaspotentialactivatorsofp53 AT nataliaalozinskaya methoxyphenylimidazolinesaspotentialactivatorsofp53 AT gelinaskopeina methoxyphenylimidazolinesaspotentialactivatorsofp53 |