Synthesis and antitumor activity of new platinum complexes

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Abstract
A new type of antitumor Pt complex was prepared and examined for antitumor activity against L1210 leukemia [mouse] both in vitro and in vivo. The coordination environment of Pt in these complexes consists of 3 anionic chloride ions and a positively charged amine. The positive charge is introduced by monoprotonation or monoalkylation of a diamine. Pt (IV) derivatives were prepared for several of the complexes, and a water-soluble sulfate derivative was prepared for one of them. Several of these complexes exhibit significant in vitro activity, and trichloro(3-aminoquinuclidinium)platinum(II) (QTP) exhibits significant in vivo activity as well. An increase in life span of .apprx. 40% was observed using QTP. QTP is toxic at doses slightly in excess of effective doses.

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