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  • 1
    Digitale Medien
    Digitale Medien
    New York, NY [u.a.] : Wiley-Blackwell
    Applied Organometallic Chemistry 11 (1997), S. 491-497 
    ISSN: 0268-2605
    Schlagwort(e): palladium ; complexes ; imidazole ; cyclometalation ; DNA ; intercalation ; drug ; Chemistry ; Industrial Chemistry and Chemical Engineering
    Quelle: Wiley InterScience Backfile Collection 1832-2000
    Thema: Chemie und Pharmazie
    Notizen: 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.
    Zusätzliches Material: 3 Ill.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 2
    ISSN: 0268-2605
    Schlagwort(e): platinum compound antileukaemic ; cytotoxic ; DNA ; thiosemicarbazone ; Chemistry ; Industrial Chemistry and Chemical Engineering
    Quelle: Wiley InterScience Backfile Collection 1832-2000
    Thema: Chemie und Pharmazie
    Notizen: 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.
    Zusätzliches Material: 1 Ill.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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