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Convenient synthesis and antiproliferative activity of 2-(Indol-2-yl)-2-arylacetamides

There have been a limited number of reports describing the preparation of 2-(indol-2-yl)-2-arylacetamides and those syntheses that have been published suffer from significant drawbacks. In addition, this class of compounds has not been evaluated biologically despite the occurrence of 2-(indol-2-yl)-...

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Главные авторы: Aksenov, D. A., Аксенов, Д. А., Kuzminov, I. K., Кузьминов, И. К., Arutiunov, N. A., Арутюнов, Н. А., Aleksandrova, E. V., Александрова, Е. В., Aksenov, A. V., Аксенов, А. В.
Формат: Статья
Язык:English
Опубликовано: Elsevier Ltd 2025
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Online-ссылка:https://dspace.ncfu.ru/handle/123456789/29804
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Описание
Краткое описание:There have been a limited number of reports describing the preparation of 2-(indol-2-yl)-2-arylacetamides and those syntheses that have been published suffer from significant drawbacks. In addition, this class of compounds has not been evaluated biologically despite the occurrence of 2-(indol-2-yl)-acetamides in natural products and medicinally important compounds. We developed a two-step synthesis of these compounds utilizing our previously developed preparation of 2-(3-oxoindolin-ylidene)-2-arylacetonitriles from o-nitroacetophenones and their transformation into the desired compounds utilizing a novel process involving treatment under mild conditions with NaBH4 in EtOH. The synthesized compounds were evaluated for antiproliferative effects against BE(2)-C neuroblastoma cells and two compounds were found to have micromolar IC50 values.