Artigo De: scopus, orcid, cienciavitae

Biophysical characterization and antineoplastic activity of new bis(thiosemicarbazonato) Cu(II) complexes

Journal of inorganic biochemistry

Palma, E.; Mendes, F.; Paulo, A.2017Elsevier

Informações chave

Autores:

Publicado em

01/02/2017

Resumo

Aiming to explore alternative mechanisms of cellular uptake and cytotoxicity, we have studied a new family of copper(II) complexes (CuL1-CuL4) with bis(thiosemicarbazone) (BTSC) ligands containing pendant protonable cyclic amines (morpholine and piperidine). Herein, we report on the synthesis and characterization of these new complexes, as well as on their biological performance (cytotoxic activity, cellular uptake, protein and DNA binding), in comparison with the parental CuIIATSM (ATSM = diacetyl-bis(N4-methylthiosemicarbazonate) complex without pendant cyclic amines. The new compounds have been characterized by a range of analytical techniques including ESI-MS, IR spectroscopy, cyclic voltammetry, reverse-phase HPLC and X-ray spectroscopy. In vitro cytotoxicity studies revealed that the copper complexes are cytotoxic, unlike the corresponding ligands, with a similar potency to that of CuATSM. Unlike CuATSM, the new complexes were able to circumvent cisplatin cross-resistance. The presence of the protonable cyclic amines did not lead to an enhancement of the interaction of the complexes with human serum albumin or calf thymus DNA. However, CuL1–CuL4 showed a remarkably augmented cellular uptake compared with CuATSM, as proved by uptake, internalization and externalization studies that were performed using the radioactive congeners 64CuL1-64CuL4. The enhanced cellular uptake of CuL1-CuL4 indicates that this new family of CuIIBTSC complexes deserves to be further evaluated in the design of metallodrugs for cancer theranostics.

Detalhes da publicação

Autores da comunidade :

Versão da publicação

AO - Versão original do autor

Editora

Elsevier

Ligação para a versão da editora

https://www.sciencedirect.com/journal/journal-of-inorganic-biochemistry

Título do contentor da publicação

Journal of inorganic biochemistry

Primeira página ou número de artigo

68

Última página

79

Volume

167

ISSN

0162-0134

WoS (Web of Science)

WOS:000392794000008

Domínio Científico (FOS)

health-sciences - Ciências de Saúde

Palavras-chave

  • charge transfer salts
  • TTF donors
  • dimercaptopyrazine bisdithiolate complexes
  • crystal engineering

Idioma da publicação (código ISO)

eng - Inglês

Identificador alternativo (URI)

http://europepmc.org/abstract/med/27907865

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