Novel triazoles of 3-acetylbetulin and betulone as anticancer agents

The CuAAC reaction of azides and acetylenic triterpenes was used for synthesis of new triazoles of 3-acetylbetulin and betulone. The triazole derivatives were evaluated for their anticancer activity in vitro against amelanotic melanoma C-32, ductal carcinoma T47D and glioblastoma SNB-19 cell lines....

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Detalles Bibliográficos
Autores principales: Bębenek, Ewa, Kadela-Tomanek, Monika, Chrobak, Elwira, Latocha, Małgorzata, Boryczka, Stanisław
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer US 2018
Materias:
Review Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6133159/
https://www.ncbi.nlm.nih.gov/pubmed/30220830
http://dx.doi.org/10.1007/s00044-018-2213-x
Descripción
Sumario:The CuAAC reaction of azides and acetylenic triterpenes was used for synthesis of new triazoles of 3-acetylbetulin and betulone. The triazole derivatives were evaluated for their anticancer activity in vitro against amelanotic melanoma C-32, ductal carcinoma T47D and glioblastoma SNB-19 cell lines. 28-[1-(3’-Deoxythymidine-5’-yl)-1H-1,2,3-triazol-4-yl]carbonylbetulone 6e exhibited a significant IC(50) value (0.17 µM) against the human glioblastoma SNB-19 cell line, an almost 5-fold higher potency while compared with reference cisplatin.

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