Synthesis, characterisation, activities, cell uptake and DNA binding of a trinuclear complex: [[trans-PtCl(NH3)]2mu-[trans-Pd(NH3)(2-hydroxypyridine)-(H2)N(CH2)6NH2)2]Cl4.

  title={Synthesis, characterisation, activities, cell uptake and DNA binding of a trinuclear complex: [[trans-PtCl(NH3)]2mu-[trans-Pd(NH3)(2-hydroxypyridine)-(H2)N(CH2)6NH2)2]Cl4.},
  author={H T Cheng and Fazlul Huq and Philip Beale and Keith J. Fisher},
  journal={European journal of medicinal chemistry},
  volume={41 7},
The trinuclear complex: [[trans-PtCl(NH3)](2)mu-[trans-Pd(NH(3))(2-hydroxypyridine)-(H(2)N(CH(2))(6)NH(2))(2)]Cl(4) (code named CH25) has been synthesized and characterized. The activity of the compound against human ovarian cancer cell lines: A2780, A2780 cisR and A2780 ZD0473R, cell up take, level of binding with DNA and nature of its interaction with pBR322 plasmid DNA have been determined. The compound is found to exhibit significant anticancer activity against the cell lines-about 45 times… Expand
Synthesis, characterization, cytotoxicity, and DNA binding of some new platinum(II) and platinum(IV) complexes with benzimidazole ligands
In this study, two Pt(II) and three Pt(IV) complexes with the structures of [PtL2Cl2] were synthesized and evaluated for their in vitro antiproliferative activities against the human MCF-7, HeLa, and HEp-2 cancer cell lines. Expand
Synthesis and Activity of a Trinuclear Platinum Complex: [{trans‐PtCl(NH3)2}2μ‐{trans‐Pt(3‐hydroxypyridine)2(H2N(CH2)6NH2)2}]Cl4 in Ovarian Cancer Cell Lines
Th1 has the potential to be developed into a highly active anticancer drug with a wider spectrum of activity than cisplatin and has been able to significantly overcome resistance in A 2780cisR and A2780ZD0473R cell lines. Expand
Neutral and ionic platinum compounds containing a cyclometallated chiral primary amine: synthesis, antitumor activity, DNA interaction and topoisomerase I-cathepsin B inhibition.
Remarkable cytotoxicity was observed for most of the synthesized Pt(ii) compounds regardless of (i) the absolute configuration R or S, and (ii) the coordinated/cyclometallated (neutral or cationic) nature of the complexes. Expand
Synthesis and structure of a new thiazoline-based palladium(II) complex that promotes cytotoxicity and apoptosis of human promyelocytic leukemia HL-60 cells
PdPyTT produced a time- and dose-dependent decrease in cell viability and increased intracellular ROS production and DNA oxidative damage, which demonstrated the promising application of palladium(II) complexes as novel anti-leukemic agents. Expand
Synthesis, characterization, antioxidant activity and DNA-binding studies of two rare earth(III) complexes with naringenin-2-hydroxy benzoyl hydrazone ligand.
Experimental evidences indicate that these three compounds can strongly bind to CT DNA via an intercalation mechanism. Expand
Kinetics and mechanism of substitution reactions of the new bimetallic [{PdCl(bipy)}{μ-(NH2(CH2)6H2N)}{PtCl(bipy)}]Cl(ClO4) complex with important bio-molecules
Abstract The new dinuclear bimetallic complex, [{PdCl(bipy)}{ μ -(NH 2 (CH 2 ) 6 H 2 N)}{PtCl(bipy)}]Cl(ClO 4 ) (bipy is 2,2′-bipyridine), has been prepared and characterized by elementalExpand
Novel Pd(II)-salen complexes showing high in vitro anti-proliferative effects against human hepatoma cancer by modulating specific regulatory genes.
The synthesis of a novel salen ligand and its mononuclear Pd-salen complexes derived from 2-hydroxy-3-{[(E)-(2-hydroxyphenyl)methylidene]amino}propyl)imino]methyl}phenol and the results suggest that Pd(II) complexes bind to DNA strongly as compared to the free ligand. Expand
Experimental and ONIOM computational evaluation of DNA- and BSA-binding and cytotoxic activity of a mononuclear Pd(II) complex with piroxicam
Abstract Binding studies of a new mononuclear Pd(II) complex, trans -[Pd(Pir) 2 ] (Pir − is piroxicam), with fish sperm deoxyribonucleic acid (FS-DNA) and bovine serum albumin (BSA) wereExpand
Phosphorus-nitrogen compounds. Part 29. Syntheses, crystal structures, spectroscopic and stereogenic properties, electrochemical investigations, antituberculosis, antimicrobial and cytotoxic activities and DNA interactions of ansa-spiro-ansa cyclotetraphosphazenes.
The mono-ferrocenyl-spiro-asa-cyclotetraphosphazenes compounds, screened for antibacterial activities against G(+) and G(-) bacteria, and for antifungal activities against yeast strains, seem to be more active against Gram positive bacteria than Gram negative. Expand


Synthesis, characterization, activities, cell uptake and DNA binding of trinuclear complex: [{trans-PtCl(NH(3))}(2)mu-{trans-Pt(NH(3))(2-hydroxypyridine)-(H(2)N(CH(2))(6)NH(2))(2)]Cl(4).
Increasing prevention of BamH1 digestion of form I and form II pBR322 plasmid DNA with the increase in concentration of CH9 provides support to the idea that global changes in DNA conformation are induced as a result of its interaction with the compound. Expand
Kinetic and equilibria studies of the aquation of the trinuclear platinum phase II anticancer agent [(trans-PtCl(NH(3))(2))(2)(mu-trans-Pt(NH(3))(2)(NH(2)(CH(2))(6)NH(2))(2))](4+) (BBR3464).
The hydrolysis profile of the bifunctional trinuclear phase II clinical agent has been examined and suggests that the dichloro form predominates. Expand
Cytotoxicity and antitumor activity of bis(platinum) complexes. A novel class of platinum complexes active in cell lines resistant to both cisplatin and 1,2-diaminocyclohexane complexes.
The in vitro cytotoxicity and in vivo antitumor activity of bis(platinum) complexes of general formula [(PtX2-(L))2H2N(CH2)nNH2] (L = NH3, X = Cl or X2 = malonato or where L = py, X = Cl) isExpand
Cooperative effects in long-range 1,4 DNA-DNA interstrand cross-links formed by polynuclear platinum complexes: an unexpected syn orientation of adenine bases outside the binding sites
Examination of the structure of the BBR3464 cross-link adduct reveals unusual cooperative effects unique to this class of anticancer drugs and is the first demonstration of cooperative effects in solution for an anticancer drug. Expand
The cellular basis of the efficacy of the trinuclear platinum complex BBR 3464 against cisplatin-resistant cells.
The cytotoxic potency and the ability of the triplatinum complex to overcome cisplatin resistance appear to be related to a different mechanism of DNA interaction (formation of different types of drug-induced DNA lesions) as compared to conventional mononuclear complexes. Expand
Comparative cytotoxicity of CI‐973, cisplatin, carboplatin and tetraplatin in human ovarian carcinoma cell lines
The results suggest that CI‐973 and teatraplatin may have potential utility in some cases of cisplatin‐resistant ovarian cancer, and are consistent with the existence of at least 2 platinum‐resistance phenotypes. Expand
Rapid colorimetric assay for cellular growth and survival: application to proliferation and cytotoxicity assays.
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A tetrazolium salt has been used to develop a quantitative colorimetric assay for mammalian cell survival and proliferation and is used to measure proliferative lymphokines, mitogen stimulations and complement-mediated lysis. Expand
Recent insights into platinum drug resistance in cancer.
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Cisplatin and its analogs have become important components of chemotherapeutic regimens for the treatment of solid tumors, however, their overall effectiveness is limited by the emergence ofExpand
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Intact and readily digestible DNA was prepared from a range of murine tissues and cell lines which had been dispersed in GHCl and ethanol precipitated, and then rinsed in 70% ethanol and resuspended in 10 mM Tris-HCl, 1 mM EDTA, pH 7.5. Expand
Structure, Recognition, and Processing of Cisplatin-DNA Adducts.