Triterpenic azines, a new class of compounds with selective cytotoxicity to leukemia cells CCRF-CEM
Language English Country England, Great Britain Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
29424548
DOI
10.4155/fmc-2017-0171
Knihovny.cz E-resources
- Keywords
- betulinic acid, cytotoxicity, hydrazone,
- 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
- Names of Substances
- Antineoplastic Agents, Phytogenic MeSH
- Hydrazines MeSH
- Triterpenes 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.
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