ChemInform Abstract: Synthesis and Antitumor Activity of Water‐Soluble 2‐Benzyl‐1,2‐ diaminobutane‐α‐oxycarboxylatoplatinum(II) Complexes.

Abstract

Synthesis and Antitumor Activity of Water-Soluble 2-Benzyl-1,2diaminobutane-α-oxycarboxylatoplatinum(II) Complexes.-The dichloroplatinum(II) complex of the title diamine shows antitumor activity accompanied by low toxicity compared to cis-platinum. However, the solubility in water has to be increased. Therefore, the chloride leaving groups are replaced by the anions of four α-hydroxycarboxylic acids. In each cage the geometrical trans/cis isomers (I) and (II) are obtained, which can be separated in the case of the lactato complexes. Starting with the racemic diamine and its corresponding enantiomers in the case of the lactato-complexes, the optical isomers are also prepared. The compounds possess a high antitumor activity toward the MDA-MB 231 mammary tumor and the P 388 leukemia of the CD2F1 mouse. -(BRUNNER, H.; MAITERTH, F.; TREITTINGER, B.; Inorg. Chim.