STRUCTURAL MODIFICATION STUDY OF BIS(SUBSTITUTED AMINOALKYLAMINO)ANTHRAQUINONES - EVALUATION OF THE RELATIONSHIP OF THE [2-[(2-HYDROXYETHYL)AMINO]ETHYL]AMINO SIDE-CHAIN WITH ANTI-NEOPLASTIC ACTIVITY

被引:113
作者
ZEECHENG, RKY [1 ]
PODREBARAC, EG [1 ]
MENON, CS [1 ]
CHENG, CC [1 ]
机构
[1] MIDWEST RES INST,KANSAS CITY,MO 64110
关键词
D O I
10.1021/jm00191a008
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Several anthraquinones containing the (2-[(2-hydroxyethyl)amino]ethyl]amino, the [2-(dimethylamino)ethyl]amino, and the 2-(dimethylamino)ethoxy groups were prepared. Preparation of a lucanthone analogue, a 7-chloroquinoline derivative, and derivatives of naphthoquinones containing the [2-[(2-hydroxyethyl)amino]ethyl]amino sidechain and related amino-substituted side chains was also conducted. It was found that the antineoplastic activity of anthraquinones containing the 12-[(2-hydroxyethyl)amino]ethyl]amino side chain is superior to those containing the tertiary amino side chain. However, the presence of the [2-[(2-hydroxyethyl)amino]ethyl]amino chain is an important, but not a sufficient, factor for good antineoplastic activity, as indicated by the lack of significant biological activity of other ring systems containing this side chain. © 1979, American Chemical Society. All rights reserved.
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页码:501 / 505
页数:5
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