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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
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Granaiola, M
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机构: Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy

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Rambaldi, M
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机构: Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy

Lenaz, G
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机构: Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy

Fato, R
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机构: Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy

Bergamini, C
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机构: Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy

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[1] Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy
[2] Univ Bologna, Dept Biochim G Moruzzi, I-40126 Bologna, Italy
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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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页码:3085 / 3089
页数:5
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