Abstract
The synthesis of diastereoisomeric [1,2-bis(2-hydroxyphenyl)ethylenediamine]dichloroplatinum(II) complexes, DL-3-PtCl2 and meso-3-PtCl2, and their evaluation on the hormone-independent, human MDA-MB231 breast cancer cell line, on the cisplatin-sensitive and -resistant L1210 leukemia cell line, on the cisplatin-resistant human NIH:OVCAR 3 ovarian cancer cell line, on the P-388 leukemia of the mouse and on the cisplatin-sensitive and -resistant Ehrlich ascites tumor of the mouse are described. On all tumor models DL-3-PtCl2 produces a marked inhibitory effect. The diastereoisomer meso-3-PtCl2 is less active and more toxic. It is striking that DL-3-PtCl2 leads to a pronounced inhibition of all cisplatin-resistant tumors. At non-toxic concentrations DL-3-PtCl2 produces cytocidal effects on the NIH:OV-CAR 3 cell line. Therefore DL-3-PtCl2 is of interest for further evaluation for the therapy of ovarian cancer.
MeSH Terms
Animals
Antineoplastic Agents/pharmacology
Carcinoma, Ehrlich Tumor/drug therapy
Cisplatin/pharmacology
Drug Resistance
Female
Humans
Mice
Organoplatinum Compounds/pharmacology
Ovarian Neoplasms/drug therapy
Tumor Cells, Cultured
Chemicals
Antineoplastic Agents
Organoplatinum Compounds
dichloro(1,2-bis(2-hydroxyphenyl)ethylenediamine)platinum II
Cisplatin
Authors & Affiliations
9 authors, click to expand affiliations / ORCID
Müller R
Institut für Pharmazie, Lehrstuhl Pharmazeutische Chemie II, Universität Regensburg, Federal Republic of Germany.
Gust R
Bernhardt G
Keller C
Schönenberger H
Seeber S
Osieka R
Eastman A
Jennerwein M
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