中国药理学通报2011，Vol.27Issue(12)：1710-1713,4.DOI:10.3969/j.issn.1001-1978.2011.12.019
3-全乙酰化半乳吡喃糖基-5-氟尿嘧啶的合成及其体外抗肿瘤活性研究
Synthesis of 3-peracetylated galactopyranosyl-5-fluorouracil and the study of its antitumor activities in vitro
摘要
Abstract
Aim To design and prepare a 5-fluoroura-cil-galactoside derivative and determine its antitumor activity in vitro. Methods Based on the molecular structure of 5-fluorouracil, 3-peracetylated galactopyr-anosyl-5-fluorouracil ( 3-PGF ) was synthesized and I-dentified using MS and 1 H-NMR. After treatments with 5-FU and 3-PGF, the growth inhibitory rates on human colon cancer cells ( SW-1116 ) and human intestinal epithelial cells ( HIEC ) were detected using MTT assay. Results The 5-fluorouracil-galactoside derivative was prepared and the structure of it was determined by MS and :H-NMR as 3-peracetylated galactopyranosyl-5-fluorouracil. And the growth inhibitory rates of 3-PGF ( 0. 01 ~ 100 umol . L-1 ) on SW-1116 cells for 48 h were 28. 45% ~ 64. 04%. At the same time, 3-PGF had lower inhibitory rates on HIEC than 5-FU. Conclusions The 5-fluorouracil-galactoside derivative, 3-peracetylated galactopyranosyl-5-fluorouracil, which was synthesized successfully in our lab , has a good antitumor activity. Furthermore, it is less toxic than 5-fluorouracil and gives some novel thoughts for design and synthesis of 5-fluorouracil derivatives.关键词
5-氟尿嘧啶/半乳糖/衍生物/3-PGF/抗肿瘤活性/毒性Key words
5-fluorouracil/ galactose/ derivative/ 3-PGF/ antitumor activity/ toxicity分类
医药卫生引用本文复制引用
黄海涛,姜茹,岳正刚,梅其炳..3-全乙酰化半乳吡喃糖基-5-氟尿嘧啶的合成及其体外抗肿瘤活性研究[J].中国药理学通报,2011,27(12):1710-1713,4.基金项目
国家科技重大专项资助项目(No 2009ZX09103-113) （No 2009ZX09103-113）
