title: 2-(aminoalkyl)-5-nitropyrazolo[3,4,5-kl]acridines, a new class of anticancer agents.
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.
authors: Warner-Lambert/Parke-Davis Pharmaceutical Research, Ann Arbor, Michigan 48106.
authors: D B
authors: DB
authors: Capps
authors: J
authors: J
authors: Dunbar
authors: S R
authors: SR
authors: Kesten
authors: J
authors: J
authors: Shillis
authors: L M
authors: LM
authors: Werbel
authors: J
authors: J
authors: Plowman
authors: D L
authors: DL
authors: Ward
mesh_terms: D000166:Acridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D000609:Aminoacridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D002460:Cell Line; D006801:Humans; D007939:Leukemia L1210 / Q000188:drug therapy; D007941:Leukemia P388 / Q000188:drug therapy; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D013329:Structure-Activity Relationship
chemical_list: D000166:Acridines; D000609:Aminoacridines; D000970:Antineoplastic Agents; D011720:Pyrazoles; C064541:NSC 366140