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 leukemi...

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Veröffentlicht in:	Journal of medicinal chemistry 1992-12, Vol.35 (26), p.4770-4778
Hauptverfasser:	Capps, David B, Dunbar, James, Kesten, Suzanne R, Shillis, Joan, Werbel, Leslie M, Plowman, Jacqueline, Ward, Donald L
Format:	Artikel
Sprache:	eng
Schlagworte:	Acridines - chemical synthesis Acridines - chemistry Acridines - therapeutic use Aminoacridines - chemical synthesis Aminoacridines - chemistry Aminoacridines - therapeutic use Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - therapeutic use Cell Line Chemistry Exact sciences and technology Heterocyclic compounds Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings Humans Leukemia L1210 - drug therapy Leukemia P388 - drug therapy Organic chemistry Preparations and properties Pyrazoles - chemical synthesis Pyrazoles - chemistry Pyrazoles - therapeutic use Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00104a001