Seven new water-soluble cationic complexes of general formula [Pt(2-pyc)(N-N)]+ (where N-N is 2NH3, ethylenediamine (en), 1,2-diaminopropane (1,2-dap), 1,3-diaminopropane (1,3-dap), (+/-) trans-1,2-diaminocyclohaxane (dach), 2,2'-dipyridylamine (dpa) or 1,10-phenanthroline (phen), and 2-pyridinecarboxylate anion) have been prepared. These complexes have been characterized by conductance measurements, and by ultraviolet-visible, infrared (IR), and 1H nuclear magnetic resonance (NMR) spectroscopy. The COSY (correlated spectroscopy) spectra of [Pt(2-pyc)(dpa)]+ and [Pt(2-pys)(dpa)]+ further support the structures of the above complexes with three nitrogen and one oxygen donor atoms in the first coordination sphere of platinum(II) with 1,2-diamine or alpha-diimine and 2-pyridinecarboxylate anion behaving as bidentate ligands. One of the compounds, [Pt(2-pyc)(dpa)]Cl, also shows a birefringence property in water. These compounds inhibit the growth of P388 lymphocytic leukemia cells. [Pt(2-pyc)(dpa)]+ shows I.D.50 value comparable to cisplatin. However, six other complexes show higher I.D.50 values than cisplatin. In addition, the inhibition studies also suggest that their target is DNA. Therefore, the interactions of four of the above complexes with calf thymus DNA have been studied by ultraviolet and fluorescence spectral methods. These studies suggest that [Pt(2-pyc)(NH3)2]+ and [Pt(2-pyc)(1,2-dap)+ bind to DNA by noncovalent interactions. On the other hand, [Pt(2-pyc)(dpa)]+ and [Pt(2-pyc)(phen)]+ bind to DNA by covalent monofunctional binding. The latter two complexes have also been interacted with PUC19 DNA. The gel electrophoresis studies of these interactions suggest that these complexes bind to DNA, and this binding leads to a conformational change in DNA.
Journal of inorganic biochemistry. 1996 Feb 15;61(3):179-96. doi: 10.1016/0162-0134(95)00055-0 Q23.22025
Synthesis, characterization, cytotoxic, and DNA binding studies of some platinum (II) complexes of 1,2-diamine and alpha-diimine with 2-pyridinecarboxylate anion
含2-吡啶甲酸根的铂(Ⅱ)金属配合物的合成、表征及其细胞毒性与DNA结合性能研究 翻译改进
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DOI: 10.1016/0162-0134(95)00055-0 PMID: 9064362
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Keywords:cytotoxic; dna binding studies
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期刊名:Journal of inorganic biochemistry
缩写:J INORG BIOCHEM
ISSN:0162-0134
e-ISSN:1873-3344
IF/分区:3.2/Q2