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N-[(N-halogenoacyl)imino]acenaphthene-quinoxalines as potential antitumoral agents.

Authors :
Boido A
Vazzana I
Sparatore F
Source :
Farmaco (Societa chimica italiana : 1989) [Farmaco] 1994 Feb; Vol. 49 (2), pp. 97-104.
Publication Year :
1994

Abstract

Applying a reaction formerly studied by the Authors between acenaphthenequinone and N1-(2-amino)phenyl-N2-acylhydrazines, a group of N-[(N-alpha- and beta- halogenoacyl)imino]acenaphthenequinoxalines were obtained. On account of the reactivity of the halogen atom, they are potentially interesting as antitumoral agents. In contrast with the beta-chloropropionyl derivative, the alpha-halogenoacyl derivatives were formed in low yields and with the simultaneous loss of the whole halogenoacylimino group. Thus, an alternative synthetic route was set up, consisting in the N-imination of acenaphthenequinoxalines by means of O-mesitylenesulfonylhydroxylamine, followed by acylation of the intermediate N-iminoacenaphthenequinoxalines. The National Cancer Institute of Bethesda evaluated the activity against lymphocytic leukemia P 388 on some of the numerous compounds now described. Only the N-chloroacetyliminoacenaphthenequinoxaline exhibited, at the dose of 50 mg/Kg i.p., 35% increase of the average survival time of treated mice. All the remaining compounds were inactive.

Details

Language :
English
ISSN :
0014-827X
Volume :
49
Issue :
2
Database :
MEDLINE
Journal :
Farmaco (Societa chimica italiana : 1989)
Publication Type :
Academic Journal
Accession number :
8003187