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[3 + 2]-Annulation of pyridinium ylides with 1-chloro-2-nitrostyrenes unveils a tubulin polymerization inhibitor

[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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محفوظ في:
التفاصيل البيبلوغرافية
المؤلفون الرئيسيون: 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.
التنسيق: Статья
اللغة:English
منشور في: Royal Society of Chemistry 2021
الموضوعات:
Indolizines
Pyrazolo[1,5-a]pyridines
Indolizine 9db
Anticancer agents
الوصول للمادة أونلاين:https://dspace.ncfu.ru/handle/20.500.12258/18098
الوسوم: إضافة وسم
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الوصف
الملخص: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

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