Seidenberger, Horst and Wappes, Beate and Schönenberger, Helmut and Beck, Wolfgang and Girnth-Weller, Michael and Ruckdeschel, Gotthart (1983) Relations between structure and antitumor activity of cis-dichloro[bis(oligopeptide ester)platinum(II)] complexes. Archiv der Pharmazie 316 (2), pp. 121-131.
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Several title compds., cis- and trans-[PtA2X2] complexes (A = esters of oligopeptides; X = Cl, oxalate, or malonate), were tested for their ability to inhibit thymidine 3H incorporation by suspensions by ADJ/PC6 plasmacytoma cells, as an index of antitumor action. The effect was markedly dependent on the type, no., and sequence of the amino acids in the peptide component. The most active compd. was cis-[Pt(Gly-GlyOEt)2Cl2] [60426-60-0], whose activity was comparable with that of mitomycin C, amethopterin, or 5-fluorouracil. The isomeric trans-[Pt(Gly-GlyOEt)2Cl2] [39680-31-4] had insignificant activity. Substitution of other amino acids for the glycyl residue directly coordinated to the Pt markedly decreased antitumor activity, as did replacement of Gly-GlyOEt by Gly-Gly-GlyOEt. There was a close correlation between the ability of the compds. to inhibit thymidine uptake in the above system and their inhibition of ADJ/PC6 plasmacytoma growth in mice. Brief data are also given on the UV difference spectra of DNA after interaction with some of the Pt compds.
|Additional information (public):||CAN 98:137216 1-3 Pharmacology 14096-51-6; 14913-33-8; 15663-27-1; 39680-31-4; 60399-28-2; 60426-60-0; 82474-57-5; 82474-58-6; 82474-59-7; 82474-60-0; 82474-61-1; 82474-62-2; 82474-63-3; 82482-19-7; 82484-32-0; 82484-33-1; 85166-35-4; 85166-36-5; 85200-51-7 Role: BAC (Biological activity or effector, except adverse), BSU (Biological study, unclassified), THU (Therapeutic use), BIOL (Biological study), USES (Uses) (neoplasm inhibition by, structure in relation to); 7440-06-4DP; 25104-18-1DP; 38000-06-5DP Role: SPN (Synthetic preparation), PREP (Preparation) (prepn. of and neoplasm inhibition by, structure in relation to); 25104-18-1 Role: RCT (Reactant), RACT (Reactant or reagent) (reaction of, with dipotassium platinum tetrachloride); 10025-99-7 Role: RCT (Reactant), RACT (Reactant or reagent) (reaction of, with polylysine)|
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Retired Professors > Prof. Schönenberger|
|Keywords:||Deoxyribonucleic acid formation (by neoplasm, platinum-peptide ester complexes inhibition of, neoplasm inhibition in relation to) Deoxyribonucleic acids Role: PRP (Properties) (interaction of, with platinum-peptide ester complexes, neoplasm inhibition in relation to) Neoplasm inhibitors (platinum-peptide ester complexes) Molecular structure-biological activity relationship (neoplasm-inhibiting, of platinum-peptide ester complexes) antitumor platinum peptide complex structure antitumor activity platinum complex|
|Subjects:||500 Science > 540 Chemistry & allied sciences|
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Deposited On:||12 Nov 2010 09:06|
|Last Modified:||12 Nov 2010 09:06|