Počet záznamů: 1
Hetero-Bis-Conjugation of Bioactive Molecules to Half-Sandwich Ruthenium(II) and Iridium(III) Complexes Provides Synergic Effects in Cancer Cell Cytotoxicity
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SYSNO ASEP 0554906 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Hetero-Bis-Conjugation of Bioactive Molecules to Half-Sandwich Ruthenium(II) and Iridium(III) Complexes Provides Synergic Effects in Cancer Cell Cytotoxicity Tvůrce(i) Biancalana, L. (IT)
Kostrhunová, Hana (BFU-R) RID, ORCID
Batchelor, L. (CH)
Hadiji, M. (CH)
Degano, I. (IT)
Pampaloni, G. (IT)
Zacchini, S. (IT)
Dyson, P.J. (CH)
Brabec, Viktor (BFU-R) RID, ORCID
Marchetti, F. (IT)Celkový počet autorů 10 Zdroj.dok. Inorganic Chemistry. - : American Chemical Society - ISSN 0020-1669
Roč. 60, č. 13 (2021), s. 9529-9541Poč.str. 13 s. Forma vydání Tištěná - P Jazyk dok. eng - angličtina Země vyd. US - Spojené státy americké Klíč. slova anticancer agents ; platinum(iv) prodrug ; crystal-structure ; rational design ; acid ; derivatives Obor OECD Organic chemistry CEP GC20-14082J GA ČR - Grantová agentura ČR Způsob publikování Omezený přístup Institucionální podpora BFU-R - RVO:68081707 UT WOS 000671099600035 EID SCOPUS 85110193018 DOI https://doi.org/10.1021/acs.inorgchem.1c00641 Anotace Four bipyridine-type ligands variably derivatized with two bioactive groups (taken from ethacrynic acid, flurbiprofen, biotin, and benzylpenicillin) were prepared via sequential esterification steps from commercial 2,2'-bipyridine-4,4'-dicarboxylic acid and subsequently coordinated to ruthenium(II) p-cymene and iridium(III) pentamethylcyclopentadienyl scaffolds. The resulting complexes were isolated as nitrate salts in high yields and fully characterized by analytical and spectroscopic methods. NMR and MS studies in aqueous solution and in cell culture medium highlighted a substantial stability of ligand coordination and a slow release of the bioactive fragments in the latter case. The complexes were assessed for their antiproliferative activity on four cancer cell lines, showing cytotoxicity to the low micromolar level (equipotent with cisplatin). Additional biological experiments revealed a multimodal mechanism of action of the investigated compounds, involving DNA metalation and enzyme inhibition. Synergic effects provided by specific combinations of metal and bioactive fragments were identified, pointing toward an optimal ethacrynic acid/flurbiprofen combination for both Ru(II) and Ir(III) complexes. Pracoviště Biofyzikální ústav Kontakt Jana Poláková, polakova@ibp.cz, Tel.: 541 517 244 Rok sběru 2022 Elektronická adresa https://pubs.acs.org/doi/10.1021/acs.inorgchem.1c00641
Počet záznamů: 1