Synthese und Antitumoraktivität von [1,2-Diamino-1-(p-hydroxy)benzyl]ethan(dichloro)platin(II)-KomplexenSynthesis and Antitumor Activity of [1,2-Diamino-1-(p-hydroxy)benzyl]ethane(dichloro)platinum(II) Complexes

Abstract
The complexes [1,2-diamino-l-(p-hydroxy)benzyl-1-(methyl, ethyl, and phenyl)]ethane-(dichloro)platinum(II) were synthesized and characterized. The benzylic p-hydroxy group of the 1,2-diaminoethane ligand leads to good water-solubility of the complexes. The ligands were synthesized in a Strecker-type reaction, starting from the corresponding p-methoxybenzylketones. The amino nitriles were reduced to the diamines. Finally, the p-methoxy groups were converted into hydroxy groups by ether cleavage. For the preparation of the complexes, K2PtCl4 was added to the ligands. The antitumor activity of the platinum(II) compounds was tested towards the human mammary carcinoma cell line MDA-MB 231. The antitumor effect depends on the substituents and increases in the series phenyl, methyl, and ethyl. As a maximum, a growth inhibition value of 77% was obtained.

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