Pd(II) and Pt(II) Complexes of 2-Phenyl- and 2-Benzyl-imidazoline: Synthesis, Structural Characterization, DNA Modification and in vitro Antileukaemic Activity

✍ Scribed by Félix Zamora; Víctor M. González; José M. Pérez; José R. Masaguer; Carlos Alonso; Carmen Navarro-Ranninger

• Publisher: John Wiley and Sons
• Year: 1997
• Tongue: English
• Weight: 139 KB
• Volume: 11
• Category: Article
• ISSN: 0268-2605
• DOI: 10.1002/(sici)1099-0739(199708)11:8<659::aid-aoc614>3.0.co;2-b

✦ Synopsis

In this paper we describe the synthesis and chemical characterization of three new Pd(II)-imidazoline complexes: [PdCl

(2), [PdCl(SEt 2 ) (C 6 H 4 -C 3 H 5 N 2 )] ( ) and [Pd(C 6 H 4 -C 3 H 5 N 2 ) (-Br)] 2 (6). We have also analyzed the DNA modifications and in vitro antileukaemic activity of these compounds and of their previously reported analogs

4. and [Pt(C 6 H 4 -C 3 H 5 N 2 )(-Cl] (7). All these compounds modify the DNA secondary structure since they alter the melting temperature (T m ) 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 r i (input molar ratio of Pd or Pt to nucleotides), compounds 3, 6 and 7 do not modify at any r i the tertiary structure of the plasmid DNA. Antileukaemic tests suggest that compounds 1, 4 and 7 exhibit important cytotoxic activity since their IC 50 values against HL-60 human leukaemic cells were below 10 g ml Ϫ1 .