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| Item type: | Article | ||||
|---|---|---|---|---|---|
| Journal or Publication Title: | European Journal of Medicinal Chemistry | ||||
| Publisher: | Elsevier | ||||
| Volume: | 28 | ||||
| Number of Issue or Book Chapter: | 2 | ||||
| Page Range: | pp. 117-127 | ||||
| Date: | 1993 | ||||
| Additional Information (public): | CAN 119:194326 78-7 Inorganic Chemicals and Reactions 14708-56-6 (Dipotassium tetraiodoplatinate(2-) Role: RCT (Reactant), RACT (Reactant or reagent) (complexation of, with bis(difluorohydroxyphenyl)ethylenediamine); 149949-23-5; 149949-24-6 Role: RCT (Reactant), RACT (Reactant or reagent) (complexation of, with platinum); 150390-77-5P; 150390-78-6P; 150567-36-5P Role: BAC (Biological activity or effector, except adverse), BSU (Biological study, unclassified), SPN (Synthetic preparation), BIOL (Biological study), PREP (Preparation) (prepn. and mammary antitumor activity of); 150447-56-6P Role: SPN (Synthetic preparation), PREP (Preparation) (prepn. and mammary antitumor activity of racemic); 150390-74-2P; 150390-75-3P; 150390-76-4P Role: BAC (Biological activity or effector, except adverse), BSU (Biological study, unclassified), SPN (Synthetic preparation), BIOL (Biological study), PREP (Preparation) (prepn. and metathesis and mammary antitumor activity of); 150447-55-5P Role: SPN (Synthetic preparation), PREP (Preparation) (prepn. and metathesis and mammary antitumor activity of racemic); 150390-73-1P Role: RCT (Reactant), SPN (Synthetic preparation), PREP (Preparation), RACT (Reactant or reagent) (prepn. and metathesis of); 150447-54-4P Role: SPN (Synthetic preparation), PREP (Preparation) (prepn. and metathesis of racemic) | ||||
| Institutions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Prof. Schönenberger | ||||
| Projects (Historical): | SFB 234 | ||||
| Identification Number: |
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| Keywords: | Neoplasm inhibitors (platinum bis(difluorohydroxyphenyl)ethylenediamine complexes, toward mammary tumors) Isomerism and Isomers (diastereo-, of platinum bis(difluorohydroxyphenyl)ethylenediamine complexes) antitumor agent platinum hydroxyphenylethylenediamine complex amine hydroxyphenylethylenedi platinum complex | ||||
| Dewey Decimal Classification: | 500 Science > 540 Chemistry & allied sciences | ||||
| Status: | Published | ||||
| Refereed: | Yes, this version has been refereed | ||||
| Created at the University of Regensburg: | Yes | ||||
| Item ID: | 17699 |
Abstract
Meso-PtLX2 (I; L = 1,2-bis(2,6-difluoro-3-hydroxyphenyl)ethylenediamine; X = 0.5SO4, NO3, PhSO3, cyclobutane-1,1-dicarboxylate (CBDC), isocitrate) and the 2 diastereomeric PtLCl2 were prepd. The influence of the leaving groups of I on several murine tumors: P388 leukemia, MTX-M3.2 breast cancer (hormone-sensitive) and MXT-Ovex breast cancer (hormone-insensitive) was studied. The compds. with ...
Abstract
Meso-PtLX2 (I; L = 1,2-bis(2,6-difluoro-3-hydroxyphenyl)ethylenediamine; X = 0.5SO4, NO3, PhSO3, cyclobutane-1,1-dicarboxylate (CBDC), isocitrate) and the 2 diastereomeric PtLCl2 were prepd. The influence of the leaving groups of I on several murine tumors: P388 leukemia, MTX-M3.2 breast cancer (hormone-sensitive) and MXT-Ovex breast cancer (hormone-insensitive) was studied. The compds. with leaving groups, which are more easily exchangeable by H2O mols. (SO42-, NO3-, PhSO3-, produced stronger tumor inhibition and also more pronounced side effects than those with moderately stable (Cl-) or stable (CBDC, isocitrate) bond leaving groups. Against the P388 leukemia, none of the tested complexes were cytotoxic to the same extent as cis-Pt(NH3)2Cl2 (II). The MXT-Ovex breast cancer, however, was strongly inhibited by meso-PtLSO4 which was even more active than II. The hormone-sensitive MXT-M3.2 breast cancer underwent 78% inhibition by the most interesting compd. of I leaving-group series (i.e. meso-PtLCl2) at the nontoxic dosage of 5 micro mol/kg. With the well-tolerated, more active diastereomer, D,L-PtLCl2, 99% inhibition of tumor growth could be achieved at a dose of 10 micro mol/kg.
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