Development of selectively acting platinum complexes

Abstract

The antitumor activity of the stereoisomers of dichloro-1,2-bis(4-hydroxyphenyl)ethylenediamineplatinum (I) was studied in vitro (on ADJ/PC6 plasmacytoma and MDA breast cancer cells) as well as in vivo (in mice bearing ADJ/PC6 plasmacytoma). Whereas (-)-I [91326-62-4] was highly active both in vivo and in vitro, the other isomers were less active; the meso isomer [91265-66-6] was more or less inactive. The 1,2-bis(4-hydroxyphenyl)ethylenediamine moiety renders these Pt complexes more selective for estrogen receptors. The antitumor activity of the (-)-isomer was not affected by diethylstilbestrol, indicating that the antitumor action of the Pt complexes is mainly due to their cytotoxic effects.