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潜在的抗肿瘤剂。37. 咪唑并[2,1-b]噻唑和新杂环体系噻唑并[2',3':2,3]咪唑并[4,5-c]喹啉胍腙的合成及抗肿瘤活性

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.

作者信息

Andreani Aldo, Granaiola Massimiliano, Leoni Alberto, Locatelli Alessandra, Morigi Rita, Rambaldi Mirella, Lenaz Giorgio, Fato Romana, Bergamini Christian, Farruggia Giovanna

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Bologna, Via Belmeloro 6, 40126 Bologna, Italy.

出版信息

J Med Chem. 2005 Apr 21;48(8):3085-9. doi: 10.1021/jm040888s.

DOI:10.1021/jm040888s
PMID:15828848
Abstract

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.

摘要

本文报道了由咪唑并[2,1 - b]噻唑以及新杂环体系噻唑并[2',3':2,3]咪唑并[4,5 - c]喹啉合成的新型胍腙及其抗肿瘤活性。这些化合物在美国国立癌症研究所作为潜在的抗肿瘤药物进行了测试。研究了2 - 氯 - 6 - (2,5 - 二甲氧基 - 4 - 硝基苯基)咪唑并[2,1 - b]噻唑 - 5 - 甲醛（41）的胍腙的作用，发现它是线粒体呼吸链复合物III的抑制剂，并且能够在HT29和HL60细胞系中诱导细胞凋亡。

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