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9-acridinyl and 2-methoxy-6-chloro-9-acridinyl derivatives of aliphatic di-, tri-, and tetraamines. Chemistry, cytostatic activity, and schistosomicidal activity.

Abstract：

:9-acridinyl derivatives of 1,6-hexanediamine, 1,8-octanediamine, bis(3-aminopropyl)amine, N,N'-bis(3-amino-propyl)piperazine, and N-ethyl-1,6-hexanediamine in the form of their hydrochlorides were prepared in high yields and converted into potential hetero bis DNA intercalating diacridines. The corresponding potential homo bis DNA intercalating reagents were prepared by heating the above amines with 9-chloroacridines. The chemical stability of the acridines was examined. Their cytostatic activity against Cloudman melanoma cells, in vitro, has been determined. The strongest cytostatic activity was observed for the acridine derivatives of the tri- and tetraamines. The schistosomicidal activity of selected acridine and diacridine derivatives against Schistosoma mansoni in mice was found to be insignificant. The S. mansoni egg development was apparently suppressed by this treatment.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Hansen JB,Langvad E,Frandsen F,Buchardt O

doi

10.1021/jm00364a028

subject

Has Abstract

pub_date

1983-10-01 00:00:00

pages

1510-4

issue

10

eissn

0022-2623

issn

1520-4804

journal_volume

26

pub_type

杂志文章

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