Issue 44, 2019
From the journal:

Dalton Transactions

Palladium(ii) complexes with thiosemicarbazones derived from pyrene as topoisomerase IB inhibitors†

Carolina G. Oliveira, ORCID logo abc   Isolda Romero-Canelón, ORCID logo cd   Monize M. Silva,e   James P. C. Coverdale, ORCID logo e   Pedro Ivo S. Maia,f   Alzir A. Batista, ORCID logo e   Silvia Castelli,g   Alessandro Desideri,*g   Peter J. Sadler ORCID logo *c  and  Victor M. Deflon ORCID logo *a  

* Corresponding authors

a São Carlos Institute of Chemistry, University of São Paulo, São Carlos, Brazil
E-mail: deflon@iqsc.usp.br

b Institute of Chemistry, Federal University of Uberlândia, Uberlândia, Brazil

c Department of Chemistry, University of Warwick, Coventry, UK

d School of Pharmacy, University of Birmingham, Birmingham, UK

e Department of Chemistry, Federal University of São Carlos, São Carlos, Brazil

f Department of Chemistry, Federal University of the Triângulo Mineiro, Uberaba, Brazil

g Department of Biology, University of Rome Tor Vergata, Via Della Ricerca Scientifica, Rome, Italy

Abstract

New palladium complexes with thiosemicarbazonate ligands derived from pyrene exhibit potent antiproliferative activity against A2780 and cisplatin-resistant A2780Cis human ovarian cancer cells, which is dependent on substituent groups of the thiosemicarbazone ligands. Cellular accumulation and distribution studies confirmed that palladium enters the cell nucleus. DNA and topoisomerase IB studies show that one complex is a potent TopIB inhibitor, with selectivity for cancer versus normal cells.

Graphical abstract: Palladium(ii) complexes with thiosemicarbazones derived from pyrene as topoisomerase IB inhibitors

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Article information

DOI
https://doi.org/10.1039/C9DT02570G
Article type
Paper
Submitted
18 Jun 2019
Accepted
24 Sep 2019
First published
30 Oct 2019
This article is Open Access
Creative Commons BY license

Dalton Trans., 2019,48, 16509-16517

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Palladium(II) complexes with thiosemicarbazones derived from pyrene as topoisomerase IB inhibitors

C. G. Oliveira, I. Romero-Canelón, M. M. Silva, J. P. C. Coverdale, P. I. S. Maia, A. A. Batista, S. Castelli, A. Desideri, P. J. Sadler and V. M. Deflon, Dalton Trans., 2019, 48, 16509 DOI: 10.1039/C9DT02570G

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