Sulfonamide derivatives of cis-imidazolines as potent p53-MDM2/MDMX protein-protein interaction inhibitors
Daniil R Bazanov
1
,
Egor V Savin
2
,
Michael D Tsymliakov
1
,
Anita I Maksutova
1
,
Sergey E Sosonyuk
1
,
Gelina S Kopeina
2
,
N A Lozinskaya
1
Publication type: Journal Article
Publication date: 2021-10-08
scimago Q2
wos Q3
SJR: 0.470
CiteScore: 5.1
Impact factor: 3.1
ISSN: 10542523, 15548120
Organic Chemistry
General Pharmacology, Toxicology and Pharmaceutics
Abstract
p53-MDM2/MDMX interaction inhibitors represent the prospective agents for targeted anticancer therapy in tumors expressing wild-type p53 protein. Imidazoline-based MDM2-targeted inhibitors of such type, nutlins, contain halogen-substituted phenyl rings, which dramatically decrease the solubility of compounds in water. The addition of suitable hydrophilic substituents in benzene rings and to imidazoline nitrogen can improve the compound’s water solubility. In this study, we have synthesized novel hydrophilic cis-2,4,5-tris(alkoxyphenyl)imidazolines and studied the influence of N-sulfonyl substituent on protein-protein interaction compared to unsubstituted alkoxy-compounds. The biological activity of the obtained compounds was studied using Western blot analysis on A549, RKO and SH-SY5Y cancer cell lines. It was found that the derivatives are able to inhibit MDM2/MDMX-p53 interaction, promote p53 stabilization and induce p21 expression in the concentrations from 500 nM.
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Total citations:
17
Citations from 2025:
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(11.76%)
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GOST
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Bazanov D. R. et al. Sulfonamide derivatives of cis-imidazolines as potent p53-MDM2/MDMX protein-protein interaction inhibitors // Medicinal Chemistry Research. 2021. Vol. 30. No. 12. pp. 2216-2227.
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Bazanov D. R., Pervushin N. V., Savin E. V., Tsymliakov M. D., Maksutova A. I., Sosonyuk S. E., Kopeina G. S., Lozinskaya N. A. Sulfonamide derivatives of cis-imidazolines as potent p53-MDM2/MDMX protein-protein interaction inhibitors // Medicinal Chemistry Research. 2021. Vol. 30. No. 12. pp. 2216-2227.
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RIS
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TY - JOUR
DO - 10.1007/s00044-021-02802-w
UR - https://doi.org/10.1007/s00044-021-02802-w
TI - Sulfonamide derivatives of cis-imidazolines as potent p53-MDM2/MDMX protein-protein interaction inhibitors
T2 - Medicinal Chemistry Research
AU - Bazanov, Daniil R
AU - Pervushin, Nikolay V
AU - Savin, Egor V
AU - Tsymliakov, Michael D
AU - Maksutova, Anita I
AU - Sosonyuk, Sergey E
AU - Kopeina, Gelina S
AU - Lozinskaya, N A
PY - 2021
DA - 2021/10/08
PB - Springer Nature
SP - 2216-2227
IS - 12
VL - 30
SN - 1054-2523
SN - 1554-8120
ER -
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BibTex (up to 50 authors)
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@article{2021_Bazanov,
author = {Daniil R Bazanov and Nikolay V Pervushin and Egor V Savin and Michael D Tsymliakov and Anita I Maksutova and Sergey E Sosonyuk and Gelina S Kopeina and N A Lozinskaya},
title = {Sulfonamide derivatives of cis-imidazolines as potent p53-MDM2/MDMX protein-protein interaction inhibitors},
journal = {Medicinal Chemistry Research},
year = {2021},
volume = {30},
publisher = {Springer Nature},
month = {oct},
url = {https://doi.org/10.1007/s00044-021-02802-w},
number = {12},
pages = {2216--2227},
doi = {10.1007/s00044-021-02802-w}
}
Cite this
MLA
Copy
Bazanov, Daniil R., et al. “Sulfonamide derivatives of cis-imidazolines as potent p53-MDM2/MDMX protein-protein interaction inhibitors.” Medicinal Chemistry Research, vol. 30, no. 12, Oct. 2021, pp. 2216-2227. https://doi.org/10.1007/s00044-021-02802-w.