期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 66, 期 -, 页码 508-515出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.06.020
关键词
Dipyrrole-polyamide; Polyamine; Cu(II) complex; DNA cleavage; Cytotoxicity
资金
- Program for New Century Excellent Talents in University [NCET-11-0920]
- Department of Education of Guangdong Province [C1030388, 2012KJCX0024]
- Guangdong Provincial Department of Science and Technology of China [2012B050100007]
- Southern Medical University
Two C-2-symmetrical dipyrrole-polyamide dimers 2 and 3 that were tethered with triethylenetetramine and spermine, respectively, and their corresponding Cu(II) complexes 2@Cu2+ and 3@Cu2+, were synthesized and fully characterized. Agarose gel electrophoresis studies on pBR322 DNA cleavage indicated that both Cu(II) complexes exhibited potent DNA-cleaving activities under physiological conditions, most probably via an oxidative mechanism. Kinetic assay indicate that 2@Cu2+ and 3@Cu2+ exhibited comparable catalytic efficiency with the Cu(II) complex of their 2,2'-(ethane-1,2-diylbis(oxy))diethanamine-tethered analog 1. The finding that compounds 2 and 3 showed higher Cu(II) ion-complexing abilities than compound 1, suggests that strong metal complexation does not necessarily lead to an enhancement in the catalytic efficiency of a DNA-cleaving agent. In addition, three Cu(II) complexes displayed moderate inhibitory activities toward three tumor cell lines. (c) 2013 Elsevier Masson SAS. All rights reserved.
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