Back to Search
Start Over
Synthesis, crystal structure, DNA-binding and cytotoxicity in vitro of novel cis-Pt(II) and trans-Pd(II) pyridine carboxamide complexes.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Dec 15; Vol. 20 (24), pp. 7250-4. Date of Electronic Publication: 2010 Oct 26. - Publication Year :
- 2010
-
Abstract
- 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)[MCl(4)] [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-[PtL(2)Cl(2)]·CH(3)OH·DMF (1) and trans-[PdL(2)Cl(2)]·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.<br /> (Copyright © 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Antineoplastic Agents chemistry
Antineoplastic Agents toxicity
Cell Line, Tumor
Coordination Complexes chemistry
Coordination Complexes toxicity
Crystallography, X-Ray
Fishes
Humans
Isomerism
Molecular Conformation
Plasmids chemistry
Spectrometry, Fluorescence
Structure-Activity Relationship
Amides chemistry
Antineoplastic Agents chemical synthesis
Coordination Complexes chemical synthesis
DNA chemistry
Palladium chemistry
Platinum chemistry
Pyridines chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 24
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21071219
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.10.097