2-(Aminoalkyl)-5-nitropyrazoloacridines, a New Class of Anticancer Agents

Article abstract of DOI:10.1021/jm00104a001

2-(Aminoalkyl)-5-nitropyrazolo<3,4,5-kl>acridines were prepared from substituted anilines via the 1-chloro-4-nitroacridones followed by condensation with <(alkylamino)alkyl>hydrazines.Impressive activity was demonstrated for the 9-hydroxy, 9-alkoxy, and 9-acyloxy analogs in vitro on a L1210 leukemia line and in vivo against the P388 leukemia.Advanced studies led to the selection of 3bbb for clinical trial.