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[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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主要な著者: 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.
フォーマット: Статья
言語:English
出版事項: Royal Society of Chemistry 2021
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オンライン・アクセス:https://dspace.ncfu.ru/handle/20.500.12258/18098
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要約: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