Q112413883
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Závěrečná zpráva o řešení grantu Interní grantové agentury MZ ČR
Přeruš. str. : il., tab., grafy ; 32 cm
Studium kardiotoxicity a potenciálních kardioprotektivních účinků nových cytostatik (benzo/c/fluoreny, Oracin) metodami kvantový chemickými, biochemickými, kardiovaskulárně farmakologickými, toxikologickými a morfiologickými u zvířat in vivo a in vitro.; Study of cardiotoxicity and potential cardioprotective effects of new cytostatic drugs (benzo/c/fluorens, Oracin) using approaches of quantal-chemistry, cardiovascular pharmacology, toxicology, biochemistry and morphology in animals in vivo and in vitro.
- MeSH
- daunomycin MeSH
- fluoreny analogy a deriváty chemická syntéza MeSH
- hodnocení léčiv MeSH
- protinádorové látky škodlivé účinky MeSH
- srdce účinky léků MeSH
- Konspekt
- Farmacie. Farmakologie
- NLK Obory
- farmacie a farmakologie
- farmacie a farmakologie
- NLK Publikační typ
- závěrečné zprávy o řešení grantu IGA MZ ČR
5-Acetoxymethyl-3-(4-bromophenyl)-2,5-dihydrofuran-2-one previously described as highly antifungally active was found to provide the corresponding 5-methylene derivative via an unusual DMSO-promoted elimination of the ester group at C5 under antifungal assay conditions. Since the latter possessed nearly the same antifungal effect as that originally reported for the former, the 5-acetoxymethyl furanone just served as a precursor of the actual antifungally active species. A few series of compounds with alkyloxy, aryloxy and alkylidene substituents at C5 of the parent furanone structure were therefore prepared and evaluated. In line with the ease of elimination of the substituent from C5, low activities of the 5-alkoxy compounds were observed. On the other hand, their 5-aryloxymethyl congeners were found to be capable of liberating the antifungally active 5-methylene furanone into the testing medium. The antifungal effect of the 5-alkylidene derivatives was highly sensitive to substitution of the alkylidene moiety; a substituent in the allylic position was necessary for a compound to retain high activity. Parallel evaluation of cytostatic activity showed moderate activities of the antifungally active derivatives against HeLa S3 and CCRF-CEM lines. Cell cycle analysis of CCRF-CEM cells following the treatment with 5-methylene-3-(4-bromophenyl)-2,5-dihydrofuran-2-one revealed that this compound is a necrotic agent.
- MeSH
- antifungální látky chemická syntéza chemie farmakologie MeSH
- apoptóza MeSH
- buněčné linie MeSH
- cytostatické látky chemická syntéza chemie farmakologie MeSH
- furany chemická syntéza chemie farmakologie MeSH
- HeLa buňky MeSH
- lidé MeSH
- mikrobiální testy citlivosti MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
