Nontoxic combretafuranone analogues with high in vitro antibacterial activity

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F18%3A10382970" target="_blank" >RIV/00216208:11160/18:10382970 - isvavai.cz</a>
Alternative codes found
RIV/68378050:_____/18:00495960 RIV/61989592:15110/18:73588060
Result on the web
<a href="http://www.sciencedirect.com/science/article/pii/S0223523417309819" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0223523417309819</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.ejmech.2017.11.078" target="_blank" >10.1016/j.ejmech.2017.11.078</a>

Result language
angličtina
Original language name
Nontoxic combretafuranone analogues with high in vitro antibacterial activity
Original language description
A library of thirty two 3,4-diphenylfuranones related to both combretastatin A-4 and antifungal 5-(acyloxymethyl)-3-(halophenyl)-2,5-dihydrofuran-2-ones was prepared. Cytotoxic effects on a panel of cancer and normal cell lines and antiinfective activity were evaluated, and the data were complemented with tests for the activation of caspase 3 and 7. High cytotoxicity was observed in some of the halogenated analogues, eg. 3-(3,4-dichlorophenyl)-4-(4-methylphenyl)-2,5-dihydrofuran-2-one with IC50 0.12-0.23 mu M, but the compounds were also highly toxic against non-malignant control cells. More importantly, notable antibacterial activity indicating G(+) selectivity has been found in the 3,4-diarylfuranone class of compounds for the first time. Hydroxymethylation of furanone C5 knocked out cytotoxic effects (up to 40 mu M) while maintaining significant activity against Staphylococcus strains in some derivatives. MIC95 of the most promising compound, 3-(4-bromophenyl)-5,5-bis(hydroxymethyl)-4-(4-methylphenyl)-2,5-dihydrofuran-2-one against S. aureus strain ATCC 6538 was 0.98 mu M (0.38 mu g/mL) and 3.9 mu M (1.52 mu g/mL) after 24 and 48 h, respectively.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30104 - Pharmacology and pharmacy

Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2018
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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