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

Author(s)

Oliveira, Carolina G. ^{[1, 2, 3]} ; Romero-Canelon, Isolda ^{[2, 4]} ; Silva, Monize M. ^[5] ; Coverdale, James P. C. ^[5] ; Maia, Pedro Ivo S. ^[6] ; Batista, Alzir A. ^[5] ; Castelli, Silvia ^[7] ; Desideri, Alessandro ^[7] ; Sadler, Peter J. ^[2] ; Deflon, Victor M. ^[1]

Affiliation

^[1] Univ Sao Paulo, Sao Carlos Inst Chem, BR-13560970 Sao Carlos, SP - Brazil

^[2] Univ Warwick, Dept Chem, Coventry CV4 7AL, W Midlands - England

^[3] Fed Univ Uberldndia, Inst Chem, BR-38400902 Uberlandia, MG - Brazil

^[4] Univ Birmingham, Sch Pharm, Birmingham B15 2TT, W Midlands - England

^[5] Univ Fed Sao Carlos, Dept Chem, BR-13565905 Sao Carlos, SP - Brazil

^[6] Univ Fed Triangulo Mineiro, Dept Chem, BR-38025140 Uberaba - Brazil

^[7] Univ Roma Tor Vergata, Dept Biol, Via Ric Sci, I-00133 Rome - Italy

• Document type: Journal article
• Source: DALTON TRANSACTIONS; v. 48, n. 44, p. 16509-16517, NOV 28 2019.
• Web of Science Citations: 12

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. (AU)

• FAPESP's process: 09/54011-8 - Acquisition of a single-crystal X-ray diffractometer for the structural analysis of small molecules and proteins
• Grantee: Victor Marcelo Deflon
• Support Opportunities: Multi-user Equipment Program