SYNTHESIS AND ANTITUMOR-ACTIVITY OF PT(II) COMPLEXES OF BENZYL-1,2-DIAMINOETHANE LIGANDS

被引：29

作者：

BRUNNER, H

HANKOFER, P

TREITTINGER, B

机构：

[1] Institut für Anorganische Chemie, Universität Regensburg, Regensburg, D-8400

来源：

CHEMISCHE BERICHTE | 1990年 / 123卷 / 05期

关键词：

1; 2‐Diaminoethanes; Antitumor activity; P388; Leukemia; Platinum(II) complexes;

D O I：

10.1002/cber.19901230515

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Twelve new diamine ligands are synthesized and characterized in which a benzyl group and another vicinal substituent or a benzyl group, a 4‐Cl‐benzyl group, and a 4‐MeO‐benzyl group, respectively, and two other geminal substituents are attached to the 1,2‐diaminoethane skeleton. The diamine ligands are transformed into the dichloroplatinum(II) complexes. The chloride ligands of four complexes are replaced by the lactate anion, α‐Cyclodextrin and polyvinylpyrrolidone are used to increase the water solubility of the Pt(II) complexes. The antitumor activity of the Pt(II) complexes is tested towards the P388 leukemia. The compounds with small alkyl substituents show antitumor activities which are much higher than the antitumor activity of cis‐platinum. Compared to the insoluble dichloro complexes, the lactate complexes and the formulations with α‐cyclodextrin and polyvinylpyrrolidone exhibit good water solubility, and no decrease of the antitumor activity is observed. Copyright © 1990 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim

引用

页码：1029 / 1038

页数：10

共 26 条

[1] SYNTHESE DANALOGUES STRUCTURAUX DE LOXYTOCINE [J].

BOISSONNAS, RA ;

GUTTMANN, S ;

JAQUENOUD, PA ;

WALLER, JP .

HELVETICA CHIMICA ACTA, 1956, 39 (05) :1421-1427

[2]

BRUNNER H, IN PRESS EUR J MED C

[3]

BRUNNER H, 1985, EUR J MED CHEM, V6, P509

[4]

FROMMING KH, 1987, DTSCH APOTH ZTG, V127, P2040

[5]

GERAN RI, 1972, CANC CHEMOTHER REP, V3, P1

[6]

GOTTLIEB JA, 1975, CANCER CHEMOTH REP 1, V59, P621

[7]

HALL LM, 1979, J INORG BIOCHEM, V11, P2520

[8]

HANKOFER P, 1989, THESIS U REGENSBURG

[9] Researches on hydantoins. L. The synthesis of hydantoins possessing the properties of hypnotics [J].

Herbert, RM ;

Johnson, TB .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1932, 54 :2463-2470

[10]

JOHNSON GL, 1966, INORG SYNTH, V8, P242

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