Library

feed icon rss

Your email was sent successfully. Check your inbox.

An error occurred while sending the email. Please try again.

Proceed reservation?

Export
  • 1
    ISSN: 0268-2605
    Keywords: palladium ; platinum ; imidazoline ; DNA ; cyclometallated complexes ; cytotoxic activity ; Chemistry ; Industrial Chemistry and Chemical Engineering
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: In this paper we describe the synthesis and chemical characterization of three new Pd(II)-imidazoline complexes: [PdCl2 (C6H5-CH2-C3H5N2)2] (2), [PdCl(SEt2) (C6H4-C3H5N2)] (5) and [Pd(C6H4-C3H5N2) (μ-Br)]2 (6). We have also analyzed the DNA modifications and in vitro antileukaemic activity of these compounds and of their previously reported analogs [Pd Cl2 (C6H5-C3H5N2)2] (1), [Pd (C6H4-C3H5N2) (μ-OAc)]2 (3), [Pd (C6H4-C3H5N2) (μ-Cl)]2 (4) and [Pt(C6H4-C3H5N2)(μ-Cl] (7). All these compounds modify the DNA secondary structure since they alter the melting temperature (Tm) of the DNA. Circular dichroism spectra indicated, moreover, that compounds 3, 5 and 6 induced higher modification on the double helix than compounds 1, 2 and 4. While compounds 1, 2 and 5 seem to induce slight changes in the electrophoretic mobility of the open and covalently closed circular forms of pUC8 DNA at high ri (input molar ratio of Pd or Pt to nucleotides), compounds 3, 6 and 7 do not modify at any ri the tertiary structure of the plasmid DNA. Antileukaemic tests suggest that compounds 1, 4 and 7 exhibit important cytotoxic activity since their IC50 values against HL-60 human leukaemic cells were below 10 μg ml-1. © 1997 John Wiley & Sons, Ltd.
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 2
    ISSN: 0268-2605
    Keywords: platinum compound antileukaemic ; cytotoxic ; DNA ; thiosemicarbazone ; Chemistry ; Industrial Chemistry and Chemical Engineering
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: p-Isopropylbenzaldehyde thiosemicarbazone (p-is.TSCN) (1) reacts with [Pt(µ-Cl)(η3-C4H7)]2 to form a dinuclear [Pt(µ-Cl)(p-is.TSCN)]2 complex (2) and a cyclometallated cluster [Pt(p-is.TSCN)]4 (3). Biological testing of these complexes against HL-60 and U-937 human leukemic cells suggest that complexes 2 and 3 may be endowed with important cytotoxic activity properties since they exhibit IC50 values (50% inhibition of cell growth) in the micromolar range, as does the clinically used drug cisplatin (cis-DDP). Analysis of the interaction of compounds 2 and 3 with DNA indicates that the kinetics of DNA platination due to compounds 2 and 3 is faster than that of cisplatin and that after 24 h of incubation most of the platinum centers are bound to DNA. Thus, it is likely that the cytotoxic activity displayed by compounds 2 and 3 may be correlated with their high level of DNA platination. Copyright © 1998 John Wiley & Sons, Ltd.
    Additional Material: 1 Ill.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 3
    Electronic Resource
    Electronic Resource
    New York, NY [u.a.] : Wiley-Blackwell
    Applied Organometallic Chemistry 11 (1997), S. 491-497 
    ISSN: 0268-2605
    Keywords: palladium ; complexes ; imidazole ; cyclometalation ; DNA ; intercalation ; drug ; Chemistry ; Industrial Chemistry and Chemical Engineering
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: In this paper, we show the synthesis of palladium(II) 4,5-phenylimidazole cyclometalated complexes. They have been characterized by IR, 1H- and 13C-NMR spectroscopy. The cyclometalated dimer compound 2 [Pd(C15H11N2)(μ-OAc)]2 and the cyclometalated monomer compound 5 [PdBr(SEt2)(C15H11N2)], having OAc and Br as leaving groups, interact with DNA, modifying its secondary structure (as measured by Tm and CD), without modifying its tertiary structure (as determined by measurement of the electrophoretic mobility in agarose gels). The monomeric compound 5 seems to be the one that induces the highest alterations in DNA secondary structure since it strongly modifies the CD spectrum of the DNA. Melting data of drug-DNA complexes suggest that, at low drug concentration, the 4,5-Imd ligand intercalates between the base pairs in the DNA molecule, increasing the Tm, while at high drug concentrations the palladium(II) centers destabilize the double helix, producing a lowering in Tm values. These results indicate that complexes containing planar structures might selectively bind to DNA that is not supercoiled, and that therefore it only has a secondary structure. © 1997 John Wiley & Sons, Ltd.
    Additional Material: 3 Ill.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
Close ⊗
This website uses cookies and the analysis tool Matomo. More information can be found here...