N-(苯并噻唑-2-基)-1-(氟苯基)-O,O-二烷基-α-氨基膦酸酯的合成、X射线晶体学分析及抗肿瘤活性
Synthesis, X-ray crystallographic analysis, and antitumor activity of N-(benzothiazole-2-yl)-1-(fluorophenyl)-O,O-dialkyl-alpha-aminophosphonates.
作者信息
Jin Linhong, Song Baoan, Zhang Guoping, Xu Ruiqing, Zhang Sumei, Gao Xingwen, Hu Deyu, Yang Song
机构信息
Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, PR China.
出版信息
Bioorg Med Chem Lett. 2006 Mar 15;16(6):1537-43. doi: 10.1016/j.bmcl.2005.12.041. Epub 2006 Jan 6.
Alpha-aminophosphonates containing benzothiazole and fluorine moiety, 4a-4m, were synthesized by Mannich-type addition in ionic liquid media with high yield and short reaction time. Their structures were established by IR, (1)H NMR, (13)C NMR, and elemental analysis. The X-ray crystallographic data of compounds 4j and 4m were provided. The newly synthesized compounds were evaluated for their anticancer activities against PC3, A431, A375, and Bcap37 cells in vitro by the MTT method. Compound 4c is highly effective against PC3 cells and moderate to A431 cells. Hence, further study is necessary to find out the potential antitumor activities.
通过曼尼希型加成反应在离子液体介质中高产率且短反应时间内合成了含苯并噻唑和氟部分的α-氨基膦酸酯4a - 4m。通过红外光谱、核磁共振氢谱、核磁共振碳谱和元素分析确定了它们的结构。提供了化合物4j和4m的X射线晶体学数据。采用MTT法体外评价了新合成化合物对PC3、A431、A375和Bcap37细胞的抗癌活性。化合物4c对PC3细胞高效，对A431细胞中度有效。因此，有必要进一步研究以发现其潜在的抗肿瘤活性。
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