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Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic acids and evaluation of cytotoxic activity of the products

2-Aryl-2-(3-indolyl)acetohydroxamic acids demonstrate promising antitumor activity, but quickly metabolize in vivo via glucuronidation of hydroxamic acid residue. In an attempt to improve their pharmacokinetics, methyl esters were synthesized via a newly developed protocol for chemoselective mono-me...

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Главные авторы: Aksenov, D. A., Аксенов, Д. А., Aksenov, A. V., Аксенов, А. В., Prityko, L. A., Притыко, Л. А., Aksenov, N. A., Аксенов, Н. А., Rubin, M. A., Рубин, М. А.
Формат: Статья
Язык:English
Опубликовано: MDPI 2022
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Online-ссылка:https://dspace.ncfu.ru/handle/20.500.12258/18612
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spelling ir-20.500.12258-186122025-02-13T09:57:46Z Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic acids and evaluation of cytotoxic activity of the products Aksenov, D. A. Аксенов, Д. А. Aksenov, A. V. Аксенов, А. В. Prityko, L. A. Притыко, Л. А. Aksenov, N. A. Аксенов, Н. А. Rubin, M. A. Рубин, М. А. Anti-cancer activity Hydroxamic acid Indoles Methylation 2-Aryl-2-(3-indolyl)acetohydroxamic acids demonstrate promising antitumor activity, but quickly metabolize in vivo via glucuronidation of hydroxamic acid residue. In an attempt to improve their pharmacokinetics, methyl esters were synthesized via a newly developed protocol for chemoselective mono-methylation of hydroxamic acids. The cytotoxicity of these derivatives against the HeLa cell line was evaluated and found to be inferior compared to the parent lead compounds. 2022-02-01T07:16:19Z 2022-02-01T07:16:19Z 2022 Статья Aksenov, D. A., Aksenov, A. V., Prityko L. A., Aksenov, N. A., Frolova L. V., Rubin, M. A. Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic acids and evaluation of cytotoxic activity of the products // MolBank. - 2022. - Том 2022. - Выпуск 1. - Номер статьи M1307. - DOI10.3390/M1307 http://hdl.handle.net/20.500.12258/18612 en MolBank application/pdf application/pdf MDPI
institution СКФУ
collection Репозиторий
language English
topic Anti-cancer activity
Hydroxamic acid
Indoles
Methylation
spellingShingle Anti-cancer activity
Hydroxamic acid
Indoles
Methylation
Aksenov, D. A.
Аксенов, Д. А.
Aksenov, A. V.
Аксенов, А. В.
Prityko, L. A.
Притыко, Л. А.
Aksenov, N. A.
Аксенов, Н. А.
Rubin, M. A.
Рубин, М. А.
Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic acids and evaluation of cytotoxic activity of the products
description 2-Aryl-2-(3-indolyl)acetohydroxamic acids demonstrate promising antitumor activity, but quickly metabolize in vivo via glucuronidation of hydroxamic acid residue. In an attempt to improve their pharmacokinetics, methyl esters were synthesized via a newly developed protocol for chemoselective mono-methylation of hydroxamic acids. The cytotoxicity of these derivatives against the HeLa cell line was evaluated and found to be inferior compared to the parent lead compounds.
format Статья
author Aksenov, D. A.
Аксенов, Д. А.
Aksenov, A. V.
Аксенов, А. В.
Prityko, L. A.
Притыко, Л. А.
Aksenov, N. A.
Аксенов, Н. А.
Rubin, M. A.
Рубин, М. А.
author_facet Aksenov, D. A.
Аксенов, Д. А.
Aksenov, A. V.
Аксенов, А. В.
Prityko, L. A.
Притыко, Л. А.
Aksenov, N. A.
Аксенов, Н. А.
Rubin, M. A.
Рубин, М. А.
author_sort Aksenov, D. A.
title Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic acids and evaluation of cytotoxic activity of the products
title_short Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic acids and evaluation of cytotoxic activity of the products
title_full Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic acids and evaluation of cytotoxic activity of the products
title_fullStr Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic acids and evaluation of cytotoxic activity of the products
title_full_unstemmed Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic acids and evaluation of cytotoxic activity of the products
title_sort methylation of 2-aryl-2-(3-indolyl)acetohydroxamic acids and evaluation of cytotoxic activity of the products
publisher MDPI
publishDate 2022
url https://dspace.ncfu.ru/handle/20.500.12258/18612
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