Novel triazoles of 3-acetylbetulin and betulone as anticancer agents
Abstract 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..
Medienart: |
E-Artikel |
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Erscheinungsjahr: |
2018 |
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Erschienen: |
2018 |
Enthalten in: |
Zur Gesamtaufnahme - volume:27 |
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Enthalten in: |
Medicinal chemistry research - 27(2018), 9 vom: 17. Juli, Seite 2051-2061 |
Sprache: |
Englisch |
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Beteiligte Personen: |
Bębenek, Ewa [VerfasserIn] |
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Links: |
Volltext [kostenfrei] |
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Themen: |
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Anmerkungen: |
© The Author(s) 2018 |
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doi: |
10.1007/s00044-018-2213-x |
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funding: |
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PPN (Katalog-ID): |
SPR000417203 |
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520 | |a Abstract 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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