2-(aminoalkyl)-5-nitropyrazolo[3,4,5-kl]acridines, a new class of anticancer agents.
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.
Capps
D B
DB
Warner-Lambert/Parke-Davis Pharmaceutical Research, Ann Arbor, Michigan 48106.
Dunbar
J
J
Kesten
S R
SR
Shillis
J
J
Werbel
L M
LM
Plowman
J
J
Ward
D L
DL
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
D000166:Acridines; D000609:Aminoacridines; D000970:Antineoplastic Agents; D011720:Pyrazoles; C064541:NSC 366140