Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 35, Issue 1, Pages 21-30Publisher
EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/S0223-5234(00)00112-4
Keywords
hypoxia-cytotoxicity; quinoxaline 1,4-di-N-oxide; solid tumour; bioreductive activation
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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-methylpiperaiin-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.
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