SYNTHESIS AND STRUCTURE-ANTITUMOR ACTIVITY RELATIONSHIP OF SULFONYL 5-FLUOROURACIL DERIVATIVES
文献类型： 外文期刊
作者： Yan, Xiaowei 1 ; Hou, Yong 2 ; Chen, Fan 1 ; Zhao, Kejian 1 ; Hu, Maolin 1 ;
作者机构： 1.Wenzhou Univ, Coll Chem & Mat Engn, Wenzhou 325027, Peoples R China
2.Sichuan Acad Agr Sci, Inst Biotechnol & Nucle Technol, Chengdu, Peoples R China
关键词： Anticancer activities;crystal structure;sulfonyl 5-fluorouracil derivatives
期刊名称：PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS （ 影响因子：1.082； 五年影响因子：0.859 ）
ISSN： 1042-6507
年卷期： 2010 年 185 卷 1 期
页码：
收录情况： SCI
摘要： Novel sulfonyl 5-fluorouracil derivatives 2 (5-fluoro-1-(arylsulfonyl) pyrimidine-2,4(1H,3H)-diones) have been synthesized via the reaction of 5-fluorouracil with sulfonyl chloride. Their chemical structures were confirmed by means of (1)HNMR, (13)C NMR, IR, mass spectra, and elemental analyses, and, in the case of 2a, its structure was established by single crystal X-ray diffraction. Some of the compounds were assayed for anticancer (HL-60 and BEL-7402 cells) activities. Structure-activity relationship (SAR) analysis discovered that the anticancer activity was related to the configuration, and that electron-withdrawing groups at 2-position or 4-position on the aryl group of arylsulfonyl derivatives of 5-fluorouracil could enhance the anticancer activity against the BEL-7402 cells.
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