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

被引：40
|
作者：
Oliveira, Carolina G. [1 ,2 ,3 ]
Romero-Canelon, Isolda [3 ,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. [3 ]
Deflon, Victor M. [1 ]
机构：
[1] Univ Sao Paulo, Sao Carlos Inst Chem, BR-13560970 Sao Carlos, SP, Brazil
[2] Fed Univ Uberldndia, Inst Chem, BR-38400902 Uberlandia, MG, Brazil
[3] Univ Warwick, Dept Chem, Coventry CV4 7AL, W Midlands, England
[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
来源：
DALTON TRANSACTIONS | 2019年 / 48卷 / 44期
基金：
巴西圣保罗研究基金会; 英国惠康基金; 英国工程与自然科学研究理事会;
关键词：
DNA; ANTICANCER; CAMPTOTHECINS; CYTOTOXICITY; FLUORESCENCE; PLATINUM(II); MECHANISM; CLEAVAGE; CELLS;
D O I：
10.1039/c9dt02570g
中图分类号：
O61 [无机化学];
学科分类号：
070301 ; 081704 ;
摘要：
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.
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页码：16509 / 16517
页数：9
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