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Triterpenic azines, a new class of compounds with selective cytotoxicity to leukemia cells CCRF-CEM
J. Pokorny, S. Krajcovicova, M. Hajduch, M. Holoubek, S. Gurska, P. Dzubak, T. Volna, I. Popa, M. Urban,
Language English Country England, Great Britain
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
29424548
DOI
10.4155/fmc-2017-0171
Knihovny.cz E-resources
- MeSH
- Cell Line MeSH
- Antineoplastic Agents, Phytogenic chemical synthesis chemistry pharmacology MeSH
- Hydrazines chemical synthesis chemistry pharmacology MeSH
- Humans MeSH
- Molecular Conformation MeSH
- Cell Proliferation drug effects MeSH
- Drug Screening Assays, Antitumor MeSH
- Triterpenes chemical synthesis chemistry pharmacology MeSH
- Dose-Response Relationship, Drug MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
AIM: From betulinic acid (1a), we synthesized 30-oxobetulinic acid (2a) that is highly cytotoxic against many cancer cell lines; however, its generic toxicity is the main obstacle in further development as cytostatic. Methodology & results: From 2a, we prepared a new class of compounds - nonsymmetrical azines and tested their in vitro cytotoxicity. All new azines with a free 28-COOH group (4a-4e) were highly and selectively cytotoxic against the T-lymphoblastic leukemia cell line CCRF-CEM and exhibited dose-dependent inhibition of RNA and DNA synthesis and other cell-cycle alterations, including the M-phase block. CONCLUSION: The potential use of azines (4a-4e) in drug development focused on hematological cancers is significantly higher than that of previously studied acids 1a and 2a.
References provided by Crossref.org
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