期刊
JOURNAL OF BIOLOGICAL INORGANIC CHEMISTRY
卷 12, 期 5, 页码 655-665出版社
SPRINGER
DOI: 10.1007/s00775-007-0214-1
关键词
antitumor agent; dinuclear platinum complex; DNA; glutathione; guanosine-5 '-monophosphate
Multinuclear Pt(II) complexes represent a novel class of antitumor agents. In this work, a dinuclear monofunctional Pt(II) complex {[cis-Pt(NH3)(2)Cl](2)(4,4'-methylenedianiline)}(NO3)(2) (1) was synthesized and characterized by H-1 NMR, electrospray mass spectrometry, and elemental analysis. The 2D [H-1, N-15] heteronuclear single quantum coherence NMR spectra of N-15-labeled 1 revealed that the cationic core of this water-soluble complex hardly hydrolyzes in aqueous solution and reacts very slowly with glutathione. Hydrolysis appears not to be an essential step for the formation of Pt-guanosine-5'-monophosphate (5'-GMP) or Pt-DNA adducts because the complex can react readily with 5'-GMP and partially transform B-DNA into its Z form. Such properties are desired to achieve the goal of enhancing cytotoxicity and lowering side effects of Pt(II) complexes. In fact, complex 1 is highly cytotoxic against the murine leukemia (P-388) and the human non-small-cell lung cancer (A-549) cell lines, and it is more cytotoxic than cisplatin at most concentrations tested.
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