Journal of Medicinal Chemistry 1992-12-25

2-(aminoalkyl)-5-nitropyrazolo[3,4,5-kl]acridines, a new class of anticancer agents.

D B Capps, J Dunbar, S R Kesten, J Shillis, L M Werbel, J Plowman, D L Ward

Index: J. Med. Chem. 35(26) , 4770-8, (1992)

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Abstract

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.