Toward anticancer gold-based compounds targeting PARP-1: a new case study

被引：12
作者：
Citta, A. [1 ]
Scalcon, V. [1 ]
Goebel, P. [2 ]
Bertrand, B. [3 ]
Wenzel, M. [4 ]
Folda, A. [1 ]
Rigobello, M. P. [1 ]
Meggers, E. [2 ]
Casini, A. [3 ,4 ]
机构：
[1] Univ Padua, Dept Biomed Sci, Via Ugo Bassi 58-b, I-35131 Padua, Italy
[2] Univ Marburg, Fachbereich Chem, Hans Meerwein Str 4, D-35043 Marburg, Germany
[3] Univ Groningen, Dept Pharmacokinet Toxicol & Targeting, Res Inst Pharm, Antonius Deusinglaan 1, NL-9713 AV Groningen, Netherlands
[4] Cardiff Univ, Sch Chem, Main Bldg,Pk Pl, Cardiff CF10 3A, S Glam, Wales
来源：
RSC ADVANCES | 2016年 / 6卷 / 82期
关键词：
MITOCHONDRIAL THIOREDOXIN REDUCTASE; HETEROCYCLIC CARBENE COMPLEXES; BIOLOGICAL-PROPERTIES; MECHANISTIC INSIGHTS; GOLD(III) COMPLEXES; INHIBITION; CANCER; AGENTS; POLY(ADP-RIBOSE); POLYMERASE;
D O I：
10.1039/c6ra11606j
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
A new gold(III) complex bearing a 2-((2,2'-bipyridin)-5-yl)-1H-benzimidazol-4-carboxamide ligand has been synthesized and characterized for its biological properties in vitro. In addition to showing promising antiproliferative effects against human cancer cells, the compound potently and selectively inhibits the zinc finger protein PARP-1, with respect to the seleno-enzyme thioredoxin reductase. The results hold promise for the design of novel gold-based anticancer agents disrupting PARP-1 function and to be used in combination therapies.
引用
收藏
页码：79147 / 79152
页数：6
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