Kristof Meelich

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Novel derivatives of the clinically established anticancer drug oxaliplatin were synthesized. Cytotoxicity of the compounds was studied in six human cancer cell lines by means of the MTT assay. Additionally, most promising complexes were also investigated in cisplatin- and oxaliplatin-resistant human cancer cell models. The therapeutic efficacy in vivo was(More)
Platinum(II) complexes with amino alcohol ligands are of growing interest as anticancer agents capable of changing their reactivity toward biomolecules at different pH values. The binding of such compounds to the transport protein, human serum albumin (HSA), under simulated physiological conditions (pH 7.4, 100mM chloride, 37 degrees C) has been studied by(More)
Extracellular acidity is a frequent pathophysiological condition of solid tumors offering possibilities for improving the tumor selectivity of molecular therapy. This might be accomplished by prodrugs with low systemic toxicity, attaining their full antitumor potency only under acidic conditions, such as bis(2-aminoalcoholato-κ²N,O)platinum(II) complexes(More)
(SP-4-2)-Bis(2-aminoethanol)dichloroplatinum(II) (KP1356) and (SP-4-2)-bis[(R)-(-)-2-aminobutanol)]dichloroplatinum(II) (KP1433) are promising cytotoxic agents capable of changing their chemical structure depending on the pH value. On the basis of this, they are supposed to be active only in or preferentially in hypoxic tumors with low pH. In this study, we(More)
Novel cis- and trans-configured bis(oxime)platinum(II) complexes have been synthesized and characterized by elemental analyses, IR, electrospray ionization mass spectrometry, multinuclear ((1)H, (13)C, and (195)Pt) NMR spectroscopy, and, in five cases, by X-ray diffraction. Their cytotoxicity was studied in the cisplatin-sensitive CH1 cell line as well as(More)
The molecular oxygen produced in photosynthesis is generated via water oxidation at a manganese-calcium cluster called the oxygen-evolving complex (OEC). While studies in biophysics, biochemistry, and structural and molecular biology are well known to provide deeper insight into the structure and workings of this system, it is often less appreciated that(More)
(SP-4-2)-Bis[(R)-(-)-2-aminobutanol-kappaN]dichloroplatinum(II) and (SP-4-2)-bis[(R)-(-)-2-aminobutanolato-kappa2N,O]platinum(II) are promising cytotoxic agents exhibiting a strongly pH-dependent rate of reaction with the DNA-modeling nucleotide guanosine 5'-monophosphate (GMP). This potential mode-of-action binding, directly correlating with cytotoxicity,(More)
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