Studies on Synthesis, Characterization, DNA Binding and Biological Activities of Two Trans-Planaramineplatinum(II) Complexes of the form PtL2R2 where L = 3-hydroxy Pyridine and R= Acetate Ligand – (Pages 4-11)

Fehmida Fasim1, Philip Beale2, Jun Qing Yu1 and Fazlul Huq1

1Discipline of Biomedical Science, Sydney Medical School, The University of Sydney, Cumberland Campus C42, 75 East Street, Lidcombe, NSW 1825, Australia; 2Sydney Cancer Centre, Concord Hospital, Sydney, NSW 2139, Australia

DOI: http://dx.doi.org/10.14205/2309-4400.2013.01.01.2

Abstract: The present study deals with the synthesis and characterization of trans-platinum(II) complexes of general formula trans-[PtL2(R)2], where L is 3-hydroxy pyridine and R is acetate ligand. The new complexes contain acetate ligands trans to the planaramine group 3-hydroxypyridine. The complexes were characterised by a combination of elemental analysis, IR, mass spectrum and 1H NMR spectroscopy. The increasing prevention of BamH1 digestion of form I and form II pBR322 plasmid DNA with the increase in concentration of the compound is believed to be due to interstrand binding that brings about global changes in DNA conformation. Acetate complexes’ activity against human ovarian cancer cell lines: A2780, A2780cisR have also been determined. The complexes show a reduced reactivity, and decrease in cytotoxic activity compared to their chloro-counterparts. Further, the complexes are better able to overcome cisplatin resistance; they therefore present an interesting class of antitumour active trans-platinum acetate complexes.

Keywords: trans-platinums, drug design, steric hindrance, DNA binding, apoptosis.