期刊
POLYHEDRON
卷 105, 期 -, 页码 89-95出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.poly.2015.12.012
关键词
Zinc(II) thiosemicarbazone complexes; DNA/protein binding; Chemical nucleases; Topoisomerase inhibitor; Anticancer agents
资金
- University Malaya through University of Malaya [RG276-14AFR, J-21002-73851, PG105-2012B]
- University Malaya [BSP/APP/0944/2013]
Two new zinc(II) complexes, Zn(chtsc-N-Me)2 and Zn(chtsc-N-Ph)(2) where chtsc = cyclohexanone thiosemicarbazone; chtsc-N-Ph = cyclohexanone N(4) -phenyl thiosemicarbazone, were isolated and characterized by X-ray crystallography. The interaction of these complexes with DNA and protein were studied using calf thymus DNA (CT -DNA) and bovine serum albumin (BSA) as the respective models, and marked activity was observed. The complexes exhibited efficient DNA cleavage activity via the oxidative pathway involving singlet oxygen as the reactive oxygen species. The topoisomerase inhibition assay showed that, even at low concentrations, both Zn(chtsc-N-Me)(2) and Zn(chtsc-N-Ph)(2) are capable of impairing enzymatic occupation of human topoisomerase-I, a significant feature of anticancer drugs. The results of in -vitro anti -proliferation tests carried out against five different human tumor cells lines gave GI(50) values lower than 5 mu g/mL, which indicates that these complexes are potentially advantageous as anticancer agents. (C) 2015 Elsevier Ltd. All rights reserved.
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