Capps D B, Dunbar J, Kesten S R, Shillis J, Werbel L M, Plowman J, Ward D L
Warner-Lambert/Parke-Davis Pharmaceutical Research, Ann Arbor, Michigan 48106.
J Med Chem. 1992 Dec 25;35(26):4770-8. 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.