[3 + 2]-Annulation of pyridinium ylides with 1-chloro-2-nitrostyrenes unveils a tubulin polymerization inhibitor
Indolizines and pyrazolo[1,5-a]pyridines were prepared via [3 + 2]-cycloaddition of pyridinium ylides to 1-chloro-2-nitrostyrenes. The synthesized molecules were evaluated for antiproliferative activities against a BE(2)-C neuroblastoma cell line with several compounds decreasing the viability of ca...
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2021
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ir-20.500.12258-180982021-09-10T07:06:55Z [3 + 2]-Annulation of pyridinium ylides with 1-chloro-2-nitrostyrenes unveils a tubulin polymerization inhibitor Aksenov, A. V. Аксенов, А. В. Arutiunov, N. A. Арутюнов, Н. А. Kirilov, N. K. Кирилов, Н. К. Aksenov, D. A. Аксенов, Д. А. Grishin, I. Y. Гришин, И. Ю. Aksenov, N. A. Аксенов, Н. А. Rubin, M. A. Рубин, М. А. Indolizines Pyrazolo[1,5-a]pyridines Indolizine 9db Anticancer agents Indolizines and pyrazolo[1,5-a]pyridines were prepared via [3 + 2]-cycloaddition of pyridinium ylides to 1-chloro-2-nitrostyrenes. The synthesized molecules were evaluated for antiproliferative activities against a BE(2)-C neuroblastoma cell line with several compounds decreasing the viability of cancer cells. Indolizine 9db showed higher potency than that of all-trans-retinoic acid, an approved cancer drug. Mechanistically, it was found to inhibit tubulin polymerization and it is thus proposed that the discovered chemistry can be exploited for the development of novel microtubule-targeting anticancer agents 2021-09-06T13:53:57Z 2021-09-06T13:53:57Z 2021 Статья Aksenov, A. V.; Arutiunov, N. A.; Kirilov, N. K.; Aksenov, D. A.; Grishin, I. Y.; Aksenov, N. A.; Wang, H.; Du, L.; Betancourt, T.; Pelly, S. C.; Kornienko, A.; Rubin, M. [3 + 2]-Annulation of pyridinium ylides with 1-chloro-2-nitrostyrenes unveils a tubulin polymerization inhibitor // Organic and Biomolecular Chemistry. - 2021. - Том 19. - Выпуск 33. - Стр.: 7234 - 7245 http://hdl.handle.net/20.500.12258/18098 en Organic and Biomolecular Chemistry application/pdf application/pdf Royal Society of Chemistry |
institution |
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language |
English |
topic |
Indolizines Pyrazolo[1,5-a]pyridines Indolizine 9db Anticancer agents |
spellingShingle |
Indolizines Pyrazolo[1,5-a]pyridines Indolizine 9db Anticancer agents Aksenov, A. V. Аксенов, А. В. Arutiunov, N. A. Арутюнов, Н. А. Kirilov, N. K. Кирилов, Н. К. Aksenov, D. A. Аксенов, Д. А. Grishin, I. Y. Гришин, И. Ю. Aksenov, N. A. Аксенов, Н. А. Rubin, M. A. Рубин, М. А. [3 + 2]-Annulation of pyridinium ylides with 1-chloro-2-nitrostyrenes unveils a tubulin polymerization inhibitor |
description |
Indolizines and pyrazolo[1,5-a]pyridines were prepared via [3 + 2]-cycloaddition of pyridinium ylides to 1-chloro-2-nitrostyrenes. The synthesized molecules were evaluated for antiproliferative activities against a BE(2)-C neuroblastoma cell line with several compounds decreasing the viability of cancer cells. Indolizine 9db showed higher potency than that of all-trans-retinoic acid, an approved cancer drug. Mechanistically, it was found to inhibit tubulin polymerization and it is thus proposed that the discovered chemistry can be exploited for the development of novel microtubule-targeting anticancer agents |
format |
Статья |
author |
Aksenov, A. V. Аксенов, А. В. Arutiunov, N. A. Арутюнов, Н. А. Kirilov, N. K. Кирилов, Н. К. Aksenov, D. A. Аксенов, Д. А. Grishin, I. Y. Гришин, И. Ю. Aksenov, N. A. Аксенов, Н. А. Rubin, M. A. Рубин, М. А. |
author_facet |
Aksenov, A. V. Аксенов, А. В. Arutiunov, N. A. Арутюнов, Н. А. Kirilov, N. K. Кирилов, Н. К. Aksenov, D. A. Аксенов, Д. А. Grishin, I. Y. Гришин, И. Ю. Aksenov, N. A. Аксенов, Н. А. Rubin, M. A. Рубин, М. А. |
author_sort |
Aksenov, A. V. |
title |
[3 + 2]-Annulation of pyridinium ylides with 1-chloro-2-nitrostyrenes unveils a tubulin polymerization inhibitor |
title_short |
[3 + 2]-Annulation of pyridinium ylides with 1-chloro-2-nitrostyrenes unveils a tubulin polymerization inhibitor |
title_full |
[3 + 2]-Annulation of pyridinium ylides with 1-chloro-2-nitrostyrenes unveils a tubulin polymerization inhibitor |
title_fullStr |
[3 + 2]-Annulation of pyridinium ylides with 1-chloro-2-nitrostyrenes unveils a tubulin polymerization inhibitor |
title_full_unstemmed |
[3 + 2]-Annulation of pyridinium ylides with 1-chloro-2-nitrostyrenes unveils a tubulin polymerization inhibitor |
title_sort |
[3 + 2]-annulation of pyridinium ylides with 1-chloro-2-nitrostyrenes unveils a tubulin polymerization inhibitor |
publisher |
Royal Society of Chemistry |
publishDate |
2021 |
url |
https://dspace.ncfu.ru/handle/20.500.12258/18098 |
work_keys_str_mv |
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