Synthesis and antitumor activity of a series of (aminoethylpyrrolidine) platinum complexes.
A series of aminoethylpyrrolidine-platinum complexes were synthesized and partially characterized for chemical structure. The leaving groups in this series of complexes were varied in an attempt to identify cytotoxic, water-soluble aminoethylpyrrolidine-platinum complexes. The cytotoxic activity was tested in vitro against L1210 cells sensitive to cis-diamminedichloroplatinum(II) (L1210/0), L1210 cells resistant to cis-diamminedichloroplatinum(II) (L1210/DDP), and L1210 cells resistant to 1,2-diaminocyclohexane platinum (L1210/DACH). The complexes were also tested for in vivo antitumor activity against L1210/0 cells injected i.p. The results of these studies indicate that the aminoethylpyrrolidine-platinum complexes have moderate antitumor activity but are cross-resistant in L1210/DDP cells. The degree of antitumor activity was dependent on the characteristic leaving group of a given complex.
Khokhar
A R
AR
Vermont Regional Cancer Center, University of Vermont, Burlington 05405.
Brown
D B
DB
McCormack
J J
JJ
Hacker
M P
MP
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D004351:Drug Resistance; D006801:Humans; D007939:Leukemia L1210 / Q000188:drug therapy; D008297:Male; D051379:Mice; D009944:Organoplatinum Compounds / Q000494:pharmacology*; D011758:Pyrroles / Q000494:pharmacology*; D012995:Solubility; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; D011758:Pyrroles