A novel calix[4]pyrrole derivative as a potential anticancer agent that forms genotoxic adducts with DNA

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dc.contributor.author Geretto, Marta
dc.contributor.author Ponassi, Marco
dc.contributor.author Casale, Martina
dc.contributor.author Pulliero, Alessandra
dc.contributor.author Cafeo, Grazia
dc.contributor.author Malagreca, Ferdinando
dc.contributor.author Profumo, Aldo
dc.contributor.author Balza, Enrica
dc.contributor.author Bersimbaev, Rakhmetkazhi
dc.contributor.author Kohnke, Franz Heinrich
dc.contributor.author Rosano, Camillo
dc.contributor.author Izzotti, Alberto
dc.date.accessioned 2020-11-24T15:58:53Z
dc.date.available 2020-11-24T15:58:53Z
dc.date.issued 2018-07-23
dc.identifier.isbn DOI: 10.1038/s41598-018-29314-9
dc.identifier.issn 2045-2322
dc.identifier.uri http://repository.enu.kz:8080/handle/data/18335
dc.description.abstract meso-(p-acetamidophenyl)-calix[4]pyrrole 3 was found to exhibit remarkable cytotoxicity towards A549 cancer cells. A comparative study including the isomer of 3 meso-(m-acetamidophenyl)-calix[4]pyrrole 5, as well as molecules containing 'fragments' of these structures, demonstrated that both the calix[4]pyrrole and the acetamidophenyl units are essential for high cytotoxicity. Although calix[4]pyrroles and other anion-complexing ionophores have recently been reported to induce apoptosis by perturbing cellular chloride concentrations, in our study an alternative mechanism has emerged, as proven by the isolation of covalent DNA adducts revealed by the 32P postlabelling technique. Preliminary pharmacokinetic studies indicate that 3 is able to cross the Blood-Brain-Barrier, therefore being a potential drug that could kill primary and brain metastatic cancer cells simultaneously ru_RU
dc.language.iso en ru_RU
dc.publisher Scientific Reports ru_RU
dc.relation.ispartofseries Volume 8;article number 11075
dc.subject host-guest chemictry ru_RU
dc.subject bis-carboxylates ru_RU
dc.subject anion ru_RU
dc.subject binding ru_RU
dc.subject apoptosis ru_RU
dc.subject receptor ru_RU
dc.subject cells ru_RU
dc.subject inhibition ru_RU
dc.subject polyamide ru_RU
dc.subject toxicity ru_RU
dc.title A novel calix[4]pyrrole derivative as a potential anticancer agent that forms genotoxic adducts with DNA ru_RU
dc.type Article ru_RU


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