Title
New quinoxalinecarbonitrile 1,4-di-N-oxide derivatives as hypoxic- cytotoxic agents
Date Issued
01 January 2000
Access level
metadata only access
Resource Type
journal article
Author(s)
Ortega M.
Morancho M.
Martínez-Crespo F.
Sainz Y.
López De Ceráin A.
Monge A.
Publisher(s)
Elsevier Masson SAS
Abstract
We report the synthesis and biological in vitro activities of 16 new 2- quinoxalinecarbonitrile 1,4-di-N-oxides. These compounds present new basic lateral chains (piperazines and anilines) in the 3 position as well as different substituents in the 6 and/or 7 positions of the quinoxaline ring. Among piperazine derivatives, 4b (a 7-chloro-3-(4-methylpiperazin-1-yl) derivative) was the most potent (P = 0.5 x 10-6 M). In general, aniline derivatives were more potent and selective than the former, compound 12b (with a 4-(methylphenyl)amino moiety in the 3 position and a chlorine atom in the 7 position) being the best one (P = 3 x 10-6 M and HCR > 16). (C) 2000 Editions scientifiques et medicales Elsevier SAS.
Start page
21
End page
30
Volume
35
Issue
1
Language
English
OCDE Knowledge area
Química medicinal
Scopus EID
2-s2.0-0034009248
PubMed ID
Source
European Journal of Medicinal Chemistry
ISSN of the container
02235234
Sponsor(s)
The authors are grateful to Gobierno de Navarra for a predoctoral grant for Miguel Ángel Ortega, to I.C.I. (Instituto de Cooperación Iberoamericana) for a predoctoral grant for María Elena Montoya, and to Proyecto X-2 of CYTED (Programa Iberoamericano de Ciencia y Tecnología para el Desarrollo). The excellent technical assistance of Ms. Elena Menéndez and Ms. Marta Ruiz is also gratefully acknowledged.
Sources of information: Directorio de Producción Científica Scopus