Synthesis and antitumor activity of new platinum complexes.
A new type of antitumor platinum complex has been prepared and examined for antitumor activity against L1210 leukemia both in vitro and in vivo. The coordination environment of platinum in these complexes consists of three anionic chloride ions and a positively charged amine. The positive charge is introduced by monoprotonation or monoalkylation of a diamine. Platinum(IV) derivatives have been prepared for several of the complexes, and a water-soluble sulfate derivative has been 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 approximately 40% has been observed using QTP. QTP is toxic at doses slightly in excess of effective doses.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D002460:Cell Line; D055598:Chemical Phenomena; D002621:Chemistry; D007939:Leukemia L1210 / Q000188:drug therapy; D008297:Male; D051379:Mice; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000494:pharmacology
D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds