Institute of Industrial Organic Chemistry, Warszawa, Poland.
Arch Pharm (Weinheim). 2011 Apr;344(4):224-30. doi: 10.1002/ardp.201000228. Epub 2011 Jan 14.
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.
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。