Literature DB >> 6620310

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

J B Hansen, E Langvad, F Frandsen, O Buchardt.   

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.

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Year:  1983        PMID: 6620310     DOI: 10.1021/jm00364a028

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  2 in total

1.  Potent inhibition of scrapie prion replication in cultured cells by bis-acridines.

Authors:  Barnaby C H May; Aaron T Fafarman; Septima B Hong; Michael Rogers; Leslie W Deady; Stanley B Prusiner; Fred E Cohen
Journal:  Proc Natl Acad Sci U S A       Date:  2003-03-07       Impact factor: 11.205

2.  Conditional drug screening shows that mitotic inhibitors induce AKT/PKB-insensitive apoptosis.

Authors:  Maria Berndtsson; Emma Hernlund; Maria C Shoshan; Stig Linder
Journal:  J Chem Biol       Date:  2009-03-31
  2 in total

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