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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,
Jazyk angličtina Země Anglie, Velká Británie
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
29424548
DOI
10.4155/fmc-2017-0171
Knihovny.cz E-zdroje
- MeSH
- buněčné linie MeSH
- fytogenní protinádorové látky chemická syntéza chemie farmakologie MeSH
- hydraziny chemická syntéza chemie farmakologie MeSH
- lidé MeSH
- molekulární konformace MeSH
- proliferace buněk účinky léků MeSH
- screeningové testy protinádorových léčiv MeSH
- triterpeny chemická syntéza chemie farmakologie MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem 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.
Citace poskytuje Crossref.org
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