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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2025
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ir-123456789-298042025-02-20T12:25:57Z Convenient synthesis and antiproliferative activity of 2-(Indol-2-yl)-2-arylacetamides 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. Acetamides Neuroblastoma Antiproliferative activity Indole Sodium borohydride 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. 2025-02-20T12:24:01Z 2025-02-20T12:24:01Z 2025 Статья Aksenov D.A., Fernandez G.E., Kuzminov I.K., Arutiunov N.A., Aleksandrova E.V., Aksenov A.V., Vernaza A., Ramirez J., Ross K., Smith J.L., Du L., Sathish P., Tantillo D.J., Kornienko A. Convenient synthesis and antiproliferative activity of 2-(Indol-2-yl)-2-arylacetamides // Tetrahedron. - 2025. - 175. - art. no. 134515. - DOI: 10.1016/j.tet.2025.134515 https://dspace.ncfu.ru/handle/123456789/29804 en Tetrahedron application/pdf application/pdf Elsevier Ltd |
| institution |
СКФУ |
| collection |
Репозиторий |
| language |
English |
| topic |
Acetamides Neuroblastoma Antiproliferative activity Indole Sodium borohydride |
| spellingShingle |
Acetamides Neuroblastoma Antiproliferative activity Indole Sodium borohydride 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. Convenient synthesis and antiproliferative activity of 2-(Indol-2-yl)-2-arylacetamides |
| description |
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. |
| format |
Статья |
| author |
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. |
| author_facet |
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. |
| author_sort |
Aksenov, D. A. |
| title |
Convenient synthesis and antiproliferative activity of 2-(Indol-2-yl)-2-arylacetamides |
| title_short |
Convenient synthesis and antiproliferative activity of 2-(Indol-2-yl)-2-arylacetamides |
| title_full |
Convenient synthesis and antiproliferative activity of 2-(Indol-2-yl)-2-arylacetamides |
| title_fullStr |
Convenient synthesis and antiproliferative activity of 2-(Indol-2-yl)-2-arylacetamides |
| title_full_unstemmed |
Convenient synthesis and antiproliferative activity of 2-(Indol-2-yl)-2-arylacetamides |
| title_sort |
convenient synthesis and antiproliferative activity of 2-(indol-2-yl)-2-arylacetamides |
| publisher |
Elsevier Ltd |
| publishDate |
2025 |
| url |
https://dspace.ncfu.ru/handle/123456789/29804 |
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