Potential antitumor agents.: 37.: Synthesis and antitumor activity of guanylhydrazones from imidazo[2,1-b]thiazoles and from the new heterocyclic system thiazolo[2′,3′:2,3]imidazo [4,5-c]quinoline

被引:84
作者
Andreani, A
Granaiola, M
Leoni, A
Locatelli, A
Morigi, R
Rambaldi, M
Lenaz, G
Fato, R
Bergamini, C
Farruggia, G
机构
[1] Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy
[2] Univ Bologna, Dept Biochim G Moruzzi, I-40126 Bologna, Italy
关键词
D O I
10.1021/jm040888s
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This paper reports synthesis and antitumor activity of new guanylhydrazones from imidazo[2,1-b]thiazoles and from the new heterocyclic system thiazolo[2 ',3 ':2,3]imidazo[4,5-c]quinoline. The compounds were tested as potential antitumor agents at the National Cancer Institute. The effect of the guanylhydrazone of 2-chloro-6-(2,5-dimethoxy-4-nitrophenyl)imidazo[2,1-b]-thiazole-5-carbaldehyde (41) was investigated, and it was found to be an inhibitor of Complex III of the mitochondrial respiratory chain and is able to induce apoptosis in the cell lines HT29 and HL60.
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收藏
页码:3085 / 3089
页数:5
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