期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 24, 页码 7250-7254出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.10.097
关键词
Pyridinecarboxamide; DNA-binding; Pt(II) and Pd(II) complexes; Cytotoxic activity
资金
- National Natural Science Foundation of China [20671064, 20971090]
- Foundation of Educational Department of Liaoning Province [20060679]
- Natural Science Foundation of Liaoning Province [20052014]
In an attempt to establish fundamental structure-activity relationships (SAR) of Pt/Pd-based anti-tumour compounds, we have recently designed monodentate pyridyl amide ligand containing central amide units which possess external metal co-ordinating pyridyl group and internal amide functionality. It was prepared in one step from commercially available compounds in moderate to good yield. Surprisingly, treatment of K-2[MCl4] [M = Pt(II), Pd(II)] with ligand N-(4-chlorophenyl)-3-pyridinecarboxamide (L) in the same reaction condition affords two different hydrogen-bonded polymers: cis-[PtL2Cl2]center dot CH3OH center dot DMF (1) and trans-[PdL2Cl2]center dot 2DMF (2). Fluorescence analysis indicates that the two complexes can bind to fish sperm DNA (FS-DNA) and gel electrophoresis assay demonstrates the ability of the complexes to cleave the pBR322 plasmid DNA. The two complexes exhibit cytotoxic specificity and significant cancer cell inhibitory rate. Furthermore, cytotoxicity values are higher in the case of cis-Pt(II) complex than trans-Pd(II) complex in four different cancer cell lines. (C) 2010 Elsevier Ltd. All rights reserved.
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