Synthesis and Study of New 5-Substituted 1-Acetyl-4-phenyl-3-pyrrolin-2-ones as Potential Antitumor Agents
Chemistry of Heterocyclic Compounds 2018
Jevgenijs Kuzņecovs, M. Vorona, I. Kanepe-Lapsa, M. Petrova, Edvards Liepiņš, Sergejs Beļakovs, A. Leonchiks, Grigorijs Veinbergs

The treatment of 1-acetyl-5-bromo-4-phenyl-3-pyrrolin-2-one with appropriate silver salts in benzene promotes the substitution of bromine with chloride, fluoride, nitrite, nitrate, and thiocyanate groups. Biological testing of the newly synthesized compounds resulted in the discovery of moderate indoleamine 2,3-dioxygenase and matrix metalloproteinase inhibiting properties for NO2 and SCN derivatives in combination with low antitumor effect in vivo. However, testing of the NO2 derivative in mice with transplanted 4T1 mammary and CT-26 mouse colon carcinomas led to a considerable decrease in tumor volume and lung metastases without undesirable toxic effects evidencing potent tumor supressing properties.


Atslēgas vārdi
5-substituted 1-acetyl-4-phenyl-3-pyrrolin-2-ones, antitumor agents
DOI
10.1007/s10593-018-2298-7
Hipersaite
https://link.springer.com/article/10.1007%2Fs10593-018-2298-7

Kuzņecovs, J., Vorona, M., Kanepe-Lapsa, I., Petrova, M., Liepiņš, E., Beļakovs, S., Leonchiks, A., Veinbergs, G. Synthesis and Study of New 5-Substituted 1-Acetyl-4-phenyl-3-pyrrolin-2-ones as Potential Antitumor Agents. Chemistry of Heterocyclic Compounds, 2018, Vol.54, No.5, 514.-519.lpp. ISSN 0009-3122. e-ISSN 1573-8353. Pieejams: doi:10.1007/s10593-018-2298-7

Publikācijas valoda
English (en)
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