期刊论文

中文

应用化学

1000-0518

2006

23

6

655-658

10.3969/j.issn.1000-0518.2006.06.016

(20025001024):湖北省武汉市青年科技"晨光计划"项目 (02140):教育部科学技术研究项目

本校为第一机构

通过N^1-（四氢呋喃-2-基）-N^3-溴代烷基-5-氟尿嘧啶（1）和硫醇钠的反应制备-N^1-（四氢呋喃-2-基）-N^3-烷基巯基烷基-5-氟尿嘧啶（2），将其氧化得9种新型N^1-（四氢呋喃-2-基）-N^3-烷基磺酰基烷基-5-氟尿嘧啶衍生物。采用^1H NMR、IR、MS和元素分析对产物结构进行了表征。初步测试了部分化合物对体外培养A-549肺癌、HCT-8结肠癌和BEl-7402肝癌细胞的抑制活性，结果表明，目标化合物对A-549有一定的抑制活性，而对另2种癌细胞的抑制活性较差。

Nine N^1-furanidin-2＇-yl-N^3-alkylsulphonylalkyl-5-fluorouracils were synthesized via the oxidations of N^1-furanidin-2＇-yl-N^3-alkylthioalkyl-5-fluorouracils 2. The intermediates 2 were prepared by the reactions of N^1 -furanidin-2＇-yl-N^3-bromoalkyl-5-fluorouracil 1 with sodium alkylsulfide. The structures of the products were confirmed by means of ^1H NMR, IR, MS and elemental analysis. The inhibitory activities of compounds 3 to A5...