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. 28-[1-(3'-Deoxythymidine-5'-yl)-1H-1,2,3-triazol-4-yl]carbonylbetulone 6e exhibited a significant IC50 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 : an international journal for rapid communications on design and mechanisms of action of biologically active agents - 27(2018), 9 vom: 01., Seite 2051-2061 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Bębenek, Ewa [VerfasserIn] |
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| Links: |
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| Themen: |
1,2,3-Triazole |
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| Anmerkungen: |
Date Revised 20.11.2019 published: Print-Electronic Citation Status PubMed-not-MEDLINE |
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| doi: |
10.1007/s00044-018-2213-x |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM288576837 |
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| 520 | |a 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 IC50 value (0.17 µM) against the human glioblastoma SNB-19 cell line, an almost 5-fold higher potency while compared with reference cisplatin | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Review | |
| 650 | 4 | |a 1,2,3-Triazole | |
| 650 | 4 | |a Anticancer activity | |
| 650 | 4 | |a Betulin | |
| 650 | 4 | |a CuAAC | |
| 650 | 4 | |a Lipophilicity | |
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| 700 | 1 | |a Chrobak, Elwira |e verfasserin |4 aut | |
| 700 | 1 | |a Latocha, Małgorzata |e verfasserin |4 aut | |
| 700 | 1 | |a Boryczka, Stanisław |e verfasserin |4 aut | |
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