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; Niukalova, Maria; Khasanov, Shokhrukh; Esaulkova, Iana; Zarubaev, Vladimir; Boltneva, Natalia; Rudakova, Elena; Kovaleva, Nadezhda; Serebryakova, Olga; Makhaeva, Galina; Valuisky, Nikita; Ibragimova, Umida; Litvinov, Roman; Babkov, Denis; Usenov, Kubanych; Chertenkov, Matvey; Pokrovsky, Mikhail; Cheresiz, Sergey; Pokrovsky, Andrey.
в: Molecular Diversity, 16.07.2024.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 - © 2024. The Author(s), under exclusive licence to Springer Nature Switzerland AG.
PY - 2024/7/16
Y1 - 2024/7/16
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.
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.
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: 129787729