9-Acridinyl and 2-Methoxy-6-chloro-9-acridinyl Derivatives of Aliphatic Di-, Tri-, and Tetraamines. Chemistry, Cytostatic Activity, and Schistosomicidal Activity

Article abstract of DOI:10.1021/jm00364a028

9-acridinyl derivatives of 1,6-hexanediamine, 1,8-octanediamine, bis(3-aminopropyl)amine, N,N'-bis(3-aminopropyl)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.