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Synthesis, in vivo and in vitro studies on the antineoplastic effect of cis-dichloro-dipeptide ester-platinum(II) complexes

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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Abstract

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.

Item Type:

Article

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

Identification Number:

Value	Type
1976:537309	Other

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

Status:

Published

Refereed:

Yes, this version has been refereed

Created at the University of Regensburg:

Unknown

Owner:

Petra Gürster

Deposited On:

22 Nov 2010 13:48