[DL-1,2-BIS(2-HYDROXYPHENYL)ETHYLENEDIAMINE]DICHLOROPLATINUM(II), A NEW COMPOUND FOR THE THERAPY OF OVARIAN-CANCER

被引:20
作者
MULLER, R
GUST, R
BERNHARDT, G
KELLER, C
SCHONENBERGER, H
SEEBER, S
OSIEKA, R
EASTMAN, A
JENNERWEIN, M
机构
[1] UNIV REGENSBURG,INST BIOCHEM & BIOPHYS,LEHRSTUHL PHARMAZEUT CHEM 2,W-8400 REGENSBURG,GERMANY
[2] STADT KRANKENHAUS LEVERKUSEN,ZENTRUM INNERE MED,MED KLIN 3,W-5090 LEVERKUSEN 1,GERMANY
[3] RHEIN WESTFAL TH AACHEN,FAK MED,MED KLIN 4,W-5100 AACHEN,GERMANY
[4] DARTMOUTH COLL,HITCHCOCK MED CTR,DARTMOUTH MED SCH,DEPT PHARMACOL & TOXICOL,HANOVER,NH 03756
关键词
dl-1,2-Bis(2-hydroxyphenyl)ethylenediamine]dichloroplatinum(II); Ovarian cancer;
D O I
10.1007/BF01612897
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
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 cisplatinresistant human NIH:OVCAR 3 ovarian cancer cell line, on the P-388 leukemia of the mouse and on the cisplatinsensitive 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. © 1990 Springer-Verlag.
引用
收藏
页码:237 / 244
页数:8
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