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新型 2-芳基-4H-3,1-苯并噻嗪的合成及抗癌活性。

Synthesis and anticancer activity of new 2-aryl-4h-3,1-benzothiazines.

机构信息

Institute of Industrial Organic Chemistry, Warszawa, Poland.

出版信息

Arch Pharm (Weinheim). 2011 Apr;344(4):224-30. doi: 10.1002/ardp.201000228. Epub 2011 Jan 14.

Abstract

New compounds of 2-aryl-4H-3,1-benzothiazine set were synthesized and tested for their antiproliferative activity as part of our research in the antitumor field. The title compounds were obtained by the reaction of aryl-modified sulfinylbis((2,4-dihydroxyphenyl)methanethione) with 2-aminobenzyl alcohols. The reaction proceeded through thiobenzanilide intermediates, which were converted to the 4H-3,1-benzothiazine fused ring by an endocyclization process. The structures of compounds were identified from elemental, IR, (1) H-NMR, (13) C-NMR, and MS spectra analyses. The cytotoxicity in vitro against four human cancer cell lines was determined. The antiproliferative properties of some compounds were more beneficial than cisplatin studied comparatively.

摘要

我们合成了一系列新的 2-芳基-4H-3,1-苯并噻嗪化合物,并测试了它们的抗增殖活性,这是我们抗肿瘤研究的一部分。标题化合物是通过芳基修饰的亚磺酰基双((2,4-二羟基苯基)甲硫基)与 2-氨基苄醇反应得到的。反应经过硫代苯甲酰苯胺中间体,通过内环化过程转化为 4H-3,1-苯并噻嗪稠环。通过元素分析、IR、(1)H-NMR、(13)C-NMR 和 MS 光谱分析确定了化合物的结构。测定了它们对四种人癌细胞系的体外细胞毒性。与顺铂相比,一些化合物的抗增殖特性更有益。

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