Abstract
BackgroundCis-planaramineplatinum(II) complexes like their trans isomers are often found to be active against cancer cell lines. The present study deals with the synthesis, characterization and determination of activity of new cis-planaramineplatinum(II) complexes.ResultsTwo cis-planaramineplatinum(II) complexes: cis-(3-hydroxypyridine)(ammine)dichloroplatinum(II) (code named AH3) and cis-(2,3-diaminopyridine)(ammine)dichloroplatinum(II) (code named AH7) have been prepared and characterised based on elemental analyses, IR, Raman, mass and 1H NMR spectral measurements. The interactions of the compounds with pBR322 plasmid DNA have been investigated and their activity against ovarian cancer cell lines: A2780, A2780cisR and A2780ZD047Rhave been determined. Like cisplatin, AH3 and AH7 are believed to form mainly monofunctional N7(G) and bifunctional intrastrand N7(G)N7(G) adducts with DNA, causing a local distortion of a DNA strand. As a result, gel mobility of the DNA changes. Both AH3 and AH7 are found to be less active than cisplatin against the three cell lines with AH3 being the more active compound of the two. The higher activity of AH3 is in line with its lower molar conductivity value corresponding to a lower degree of dissociation.ConclusionThe differences in activity of AH3, AH7 and cisplatin against the cell lines illustrate structure-activity relationship.
Highlights
Cis-planaramineplatinum(II) complexes like their trans isomers are often found to be active against cancer cell lines
The lower molar conductivity values of AH3 and AH7 as compared to cisplatin suggests that the degree of dissociation of the compounds is less than that for cisplatin. This is in line with the presence of a bulkier planaramine ligand in AH3 and AH7 that introduces a greater steric hindrance
AH3 is found to be more active than AH7 against the three cell lines
Summary
Cis-planaramineplatinum(II) complexes like their trans isomers are often found to be active against cancer cell lines. In an attempt to reduce toxicity and widen the spectrum of activity thousands of cisplatin analogues have been prepared by varying the nature of the leaving groups and the carrier ligands [8]. BMC Chemical Biology 2006, 6:3 http://www.biomedcentral.com/1472-6769/6/3 toxicity (eg substitution of the more stable cyclobutanedicarboxylate for the two chlorides led to the development of carboplatin which produces substantially less nausea, vomiting and neurotoxicity but causes more of myelosuppression) and that of the carrier ligands, it has been possible to achieve a limited change in the spectrum of activity (eg oxaliplatin which has 1,2-diaminocyclohexane as the carrier ligands has been found to be active against colorectal cancer whilst cisplatin is not) [9,10,11].
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