Artigo De: scopus, orcid, cienciavitae
Anticancer Activity and Mode of Action of Copper(II)-Bis(thiosemicarbazonato) Complexes with Pendant Nitrogen Heterocycles
European Journal of Inorganic Chemistry
2021 — European Chemical Societies Publishing
—Informações chave
Autores:
Publicado em
15/04/2021
Resumo
Exploring the potential of bis(thiosemicarbazones) (BTSC), a new family of BTSC ligands derived from GTSM (glyoxal-bis(N4-methylthiosemicarbazonato) and respective CuIIBTSC complexes were synthesized. These complexes, having pendant nitrogen heterocycles, exhibited increased water-solubility, lower lipophilicity at physiological pH and more negative Cu(II)/Cu(I) redox potential, when compared with the parental complex. The cytotoxic evaluation performed in a panel of cancer cells lines showed an important effect of the metal complexation, and furthermore correlated well with the cellular uptake of the compounds, which was determined using their 64Cu congeners. The radiolabelling of the complexes also allowed more detailed uptake studies, with the results suggesting an active transport or facilitated diffusion mechanism for the cellular uptake of 64CuGTSMpip and 64CuGTSMmor, with pendant piperidine and morpholine rings, respectively. Additionally, a comparative study with the corresponding Cu(II) complexes derived from ATSM (diacetyl-bis(N4-methylthiosemicarbazonato) that we have previously described, demonstrated a clear difference in their lysosomotropic properties in particular for the piperidine derivatives. From this study, CuGTSMpip emerged as the most promising compound to be further evaluated as an anticancer metallodrug.
Detalhes da publicação
Autores da comunidade :
Elisa Vaz Morgado de Palma
ist423985
Paula Dolores Galhofas Raposinho
ist25382
Maria Dulce Jesus Pombo Belo
ist171949
António Manuel Rocha Paulo
ist126677
Filipa Fernandes Mendes
ist25493
Versão da publicação
AO - Versão original do autor
Editora
European Chemical Societies Publishing
Título do contentor da publicação
European Journal of Inorganic Chemistry
Primeira página ou número de artigo
1337
Última página
1348
Volume
2021
Fascículo
14
ISSN
1434-1948
WoS (Web of Science)
Domínio Científico (FOS)
chemical-sciences - Química
Idioma da publicação (código ISO)
eng - Inglês
Identificador alternativo (URI)
http://dx.doi.org/10.1002/ejic.202100168
Acesso à publicação:
Acesso apenas a metadados