Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
Efficient synthesis and evaluation of therapeutic potential of fluorine containing 2-arylchromen-4-ones. / Troshkova, Nadezhda; Politanskaya, Larisa; Wang, Jiaying и др.
в: Molecular Diversity, 22.07.2024.Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
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TY - JOUR
T1 - Efficient synthesis and evaluation of therapeutic potential of fluorine containing 2-arylchromen-4-ones
AU - Troshkova, Nadezhda
AU - Politanskaya, Larisa
AU - Wang, Jiaying
AU - Niukalova, Maria
AU - Khasanov, Shokhrukh
AU - Esaulkova, Iana
AU - Zarubaev, Vladimir
AU - Boltneva, Natalia
AU - Rudakova, Elena
AU - Kovaleva, Nadezhda
AU - Serebryakova, Olga
AU - Makhaeva, Galina
AU - Valuisky, Nikita
AU - Ibragimova, Umida
AU - Litvinov, Roman
AU - Babkov, Denis
AU - Usenov, Kubanych
AU - Chertenkov, Matvey
AU - Pokrovsky, Mikhail
AU - Cheresiz, Sergey
AU - Pokrovsky, Andrey
N1 - This work was funded by Russian Science Support Foundation, 23-23-00008.
PY - 2024/7/22
Y1 - 2024/7/22
N2 - A large series of 2-arylchromen-4-ones containing from 1 to 3 fluorine atoms or a trifluoromethyl group in the structure was synthesized by condensation of fluorinated 2-hydroxyacetophenones with benzaldehydes in an alkaline medium and subsequent oxidative cyclization of the resulting 2’-hydroxychalcones by action of I2 in DMSO. The cytotoxicity of the obtained compounds was studied in glioblastoma cell line, SNB19, and in a monkey-derived normal kidney epithelium cell line, Vero. In addition, antiglycation activity of the obtained compounds was evaluated. The inhibitory activity of some fluorinated 2-arylchromen-4-ones against acetylcholinesterase, butyrylcholinesterase and carboxylesterase as well their primary antioxidant activity in ABTS and FRAP tests were investigated. Screening of the synthesized compounds for their inhibitory activity against influenza A virus A/Puerto Rico/8/34 (H1N1) in the MDCK cell culture revealed that fluorinated compounds 32, 31 and 39 showed manifest antiviral effects (with IS = 57, 38 and 25 correspondingly) that makes this series of new biologically attractive fluorinated heterocycles promising for further development and in-depth study. Graphical abstract: A series of new fluorine-contained 2-aryl-chromen-4-one derivatives were synthesized as potential multi-targets bioactive compounds, among which 32, 31 and 39 were found to be the most promising antiviral agents. (Figure presented.)
AB - A large series of 2-arylchromen-4-ones containing from 1 to 3 fluorine atoms or a trifluoromethyl group in the structure was synthesized by condensation of fluorinated 2-hydroxyacetophenones with benzaldehydes in an alkaline medium and subsequent oxidative cyclization of the resulting 2’-hydroxychalcones by action of I2 in DMSO. The cytotoxicity of the obtained compounds was studied in glioblastoma cell line, SNB19, and in a monkey-derived normal kidney epithelium cell line, Vero. In addition, antiglycation activity of the obtained compounds was evaluated. The inhibitory activity of some fluorinated 2-arylchromen-4-ones against acetylcholinesterase, butyrylcholinesterase and carboxylesterase as well their primary antioxidant activity in ABTS and FRAP tests were investigated. Screening of the synthesized compounds for their inhibitory activity against influenza A virus A/Puerto Rico/8/34 (H1N1) in the MDCK cell culture revealed that fluorinated compounds 32, 31 and 39 showed manifest antiviral effects (with IS = 57, 38 and 25 correspondingly) that makes this series of new biologically attractive fluorinated heterocycles promising for further development and in-depth study. Graphical abstract: A series of new fluorine-contained 2-aryl-chromen-4-one derivatives were synthesized as potential multi-targets bioactive compounds, among which 32, 31 and 39 were found to be the most promising antiviral agents. (Figure presented.)
KW - Anti-glycation activity
KW - Anti-influenza virus activity
KW - Cytotoxicity
KW - Esterase profile
KW - Fluorinated flavones
UR - https://www.scopus.com/record/display.uri?eid=2-s2.0-85198736110&origin=inward&txGid=d4ccfc673460d88c90f6c05fabe7cbfc
UR - https://www.elibrary.ru/item.asp?id=68864489
UR - https://www.webofscience.com/wos/woscc/full-record/WOS:001269331800001
UR - https://www.mendeley.com/catalogue/a9e19516-c438-30e1-91e5-16cdb3f1a616/
U2 - 10.1007/s11030-024-10925-6
DO - 10.1007/s11030-024-10925-6
M3 - Article
C2 - 39012566
JO - Molecular Diversity
JF - Molecular Diversity
SN - 1381-1991
ER -
ID: 61239014