Insight into the anticancer activity of copper(Ii) 5-methylenetrimethylammonium-thiosemicarbazonates and their interaction with organic cation transporters
Închide
Conţinutul numărului revistei
Articolul precedent
Articolul urmator
589 0
SM ISO690:2012
MILUNOVIC, Miljan, PALAMARCIUC, Oleg, SÎRBU, Angela, SHOVA, Sergiu, ARION, Vladimir. Insight into the anticancer activity of copper(Ii) 5-methylenetrimethylammonium-thiosemicarbazonates and their interaction with organic cation transporters. In: Biomolecules, 2020, nr. 9(10), pp. 1-30. ISSN 2218-273X. DOI: https://doi.org/10.3390/biom10091213
EXPORT metadate:
Google Scholar
Crossref
CERIF

DataCite
Dublin Core
Biomolecules
Numărul 9(10) / 2020 / ISSN 2218-273X /ISSNe 2218-273X

Insight into the anticancer activity of copper(Ii) 5-methylenetrimethylammonium-thiosemicarbazonates and their interaction with organic cation transporters

DOI: https://doi.org/10.3390/biom10091213

Pag. 1-30

Milunovic Miljan1, Palamarciuc Oleg2, Sîrbu Angela2, Shova Sergiu3, Arion Vladimir1
 
1 University of Vienna,
2 Moldova State University,
3 “Petru Poni” Institute of Macromolecular Chemistry
 
Disponibil în IBN: 5 septembrie 2020


Rezumat

A series of four water-soluble salicylaldehyde thiosemicarbazones with a positively charged trimethylammonium moiety ([H2LR]Cl, R = H, Me, Et, Ph) and four copper(II) complexes [Cu(HLR)Cl]Cl (1–4) were synthesised with the aim to study (i) their antiproliferative activity in cancer cells and, (ii) for the first time for thiosemicarbazones, the interaction with membrane transport proteins, specifically organic cation transporters OCT1–3. The compounds were comprehensively characterised by analytical, spectroscopic and X-ray diffraction methods. The highest cytotoxic effect was observed in the neuroblastoma cell line SH-5YSY after 24 h exposure and follows the rank order: 3 > 2 > 4 > cisplatin > 1 >>[H2LR]Cl. The copper(II) complexes showed marked interaction with OCT1–3, comparable to that of well-known OCT inhibitors (decynium 22, prazosin and corticosterone) in the cell-based radiotracer uptake assays. The work paves the way for the development of more potent and selective anticancer drugs and/or OCT inhibitors.

Cuvinte-cheie
Copper(II) complexes, cytotoxicity, Organic cation transporters (OCT1–3), inhibitors, Thiosemicarbazones