Beck, Wolfgang and Purucker, Bernhard and Girnth, Michael and Schönenberger, Helmut and Seidenberger, Horst and Ruckdeschel, Gotthard (1976) Synthesis, in vivo and in vitro studies on the antineoplastic effect of cis-dichloro-dipeptide ester-platinum(II) complexes. Zeitschrift für Naturforschung B: Anorganische Chemie, organische Chemie 31B (6), pp. 832-845.
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Cis-Cl2Pt(GlyGlyOEt)2 (I) [60426-60-0] (1.7 * 10-5M) inhibited DNA formation by sarcoma 180, Yoshida sarcoma, and Walker 256 carcinosarcoma in vitro. RNA and protein synthesis were inhibited to a lesser extent. I inhibited growth of Walker 256 carcinosarcoma by 78% at 380 mg/kg i.p. in rats and produced 30% cures; I was less effective against the other tumors in vivo. I caused filamentous growth of Escherichia coli B. A DNA polymerase-deficient strain of E. coli was more strongly inhibited by I than a nondeficient strain. I was prepd. either (1) directly from K2PtCl4 and the dipeptide ester or (2) from the alpha -amino acid complex using Pt as an amino protecting group. Also prepd. Cl2Pt(MetGlyOEt) (II) [60399-21-5], Cl2Pt(ethynyl-GlyOEt) [60399-23-7], cis-Cl2Pt(GlySerOet)2 [60399-28-2], and some corresponding Pd complexes.
|Additional information (public):||CAN 85:137309 1-5 Pharmacodynamics 15663-27-1 Role: BAC (Biological activity or effector, except adverse), BSU (Biological study, unclassified), THU (Therapeutic use), BIOL (Biological study), USES (Uses) (neoplasm inhibition by, dichlorodipeptide ester platinum complexes in relation to); 60426-60-0P Role: SPN (Synthetic preparation), PREP (Preparation) (prepn. and neoplasm inhibitory activity of); 60399-15-7P; 60399-17-9P; 60399-19-1P; 60399-21-5P; 60399-23-7P; 60399-28-2P; 60399-29-3P; 60399-30-6P; 60554-12-3P Role: SPN (Synthetic preparation), PREP (Preparation) (prepn. of); 60426-61-1 Role: BIOL (Biological study) (reaction with amino acid ethyl esters); 459-73-4 Role: BIOL (Biological study) (reaction with amino acid platinum complexes); 10025-99-7 Role: BIOL (Biological study) (reaction with dipeptide ethyl esters); 15654-65-6; 15654-80-5; 21434-59-3 Role: BIOL (Biological study) (reaction with glycine ethyl ester); 26348-61-8 Role: BIOL (Biological study) (reaction with glycine nitrophenol ester platinum complex); 100-02-7 Role: BIOL (Biological study) (reaction with glycine platinum complex); 17567-45-2 Role: BIOL (Biological study) (reaction with nitrophenol); 2087-41-4; 60392-15-6 Role: BIOL (Biological study) (reaction with potassium chloroplatinate)|
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Retired Professors > Prof. Schönenberger|
|Keywords:||Bactericides, Disinfectants and Antiseptics Neoplasm inhibitors (dichlorodipeptide ester platinum complexes) Deoxyribonucleic acids Proteins Ribonucleic acids Role: FORM (Formation, nonpreparative) (formation of, by neoplasm, dichlorodipeptide ester platinum complex inhibition of) peptide platinum complex neoplasm inhibitor|
|Subjects:||500 Science > 540 Chemistry & allied sciences|
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Unknown|
|Deposited On:||22 Nov 2010 12:48|
|Last Modified:||22 Nov 2010 12:48|