PREPARATION, CHARACTERIZATION AND THE ANTICANCER ACTIVITY OF A NOVEL SERIES OF TRIAMINEMONOCHLOROPLATINUM(II) CATIONS LINKED TO ANTHRAQUINONE INTERCALATORS

被引：16

作者：

GEAN, KF

BENSHOSHAN, R

RAMU, A

RINGEL, I

KATZHENDLER, J

GIBSON, D

机构：

[1] HEBREW UNIV JERUSALEM, SCH PHARM, DEPT PHARMACEUT CHEM, JERUSALEM, ISRAEL

[2] HEBREW UNIV JERUSALEM, SCH PHARM, DEPT PHARMACOL, JERUSALEM, ISRAEL

[3] HADASSAH UNIV HOSP, DEPT RADIAT & CLIN ONCOL, JERUSALEM, ISRAEL

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 26卷 / 06期

关键词：

PLATINUM; TRIAMINEMONOCHLORO; ANTHRAQUINONE; STRUCTURE ACTIVITY RELATIONSHIPS;

D O I：

10.1016/0223-5234(91)90193-Q

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of complexes of the type [PtAm2LCl]+ (where Am = NH3 or Am2 = ethylenediamine and L is a monodentate AQ-Y-(CH2)n-NH2, AQ = anthraquinone, Y = NH, O) was prepared and screened in vitro against P388 leukemia. These complexes displayed higher activities than the corresponding neutral PtAm2L2 1:2 Pt:anthraquinone complexes but lower than the neutral diaminedichloro 1:1 complexes. The [Pt(en)LCl]+ complexes were significantly less active than the cis- and trans-[Pt(NH3)2LCl]+ complexes. The cis and trans isomers displayed similar activities. The complexes bearing the shorter linker chains were more active than those with longer chains. In vivo toxicity studies indicate that they are significantly less toxic than cis-DDP.

引用

页码：593 / 598

页数：6

共 33 条

[1] SYNTHESIS AND DNA-BINDING AND PHOTONICKING PROPERTIES OF ACRIDINE-ORANGE LINKED BY A POLYMETHYLENE TETHER TO (1,2-DIAMINOETHANE)DICHLOROPLATINUM(II) [J].