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New quinoxalinecarbonitrile 1,4-di-N-oxide derivatives as hypoxic-cytotoxic agents.

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 x10(-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) 16).

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Ortega MA,Morancho MJ,Martínez-Crespo FJ,Sainz Y,Montoya ME,López de Ceráin A,Monge A

doi

10.1016/s0223-5234(00)00112-4

subject

Has Abstract

pub_date

2000-01-01 00:00:00

pages

21-30

issue

1

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(00)00112-4

journal_volume

35

pub_type

杂志文章

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