Synthesis and Antitumor Activity of Capecitabine Derivatives

被引：2

作者：

Jia Xuedong ^{[1
,2
,3
]}

Liu Xiujun ^{[1
,2
]}

Wang Jian ^{[4
]}

Wang Minghua ^{[1
,2
]}

Guo Huiyuan ^{[1
,2
]}

Liu Mingliang ^{[1
,2
]}

机构：

[1] Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China

[2] Peking Union Med Coll, Beijing 100050, Peoples R China

[3] Zhengzhou Univ, Affiliated Hosp 1, Zhengzhou 450052, Peoples R China

[4] 5 Hosp Harbin, Harbin 150040, Peoples R China

来源：

CHEMICAL RESEARCH IN CHINESE UNIVERSITIES | 2015年 / 31卷 / 01期

基金：

中国国家自然科学基金;

关键词：

Capecitabine; Derivative; Antitumor activity; PRODRUG; DESIGN; AGENTS; COST;

D O I：

10.1007/s40242-015-4282-4

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of capecitabine derivatives with a Boc group at the N-4-position was synthesized and their in vitro antitumor activities against HepG2(liver hepatocellular carcinoma) were primarily evaluated. Some compounds were chosen for further evaluation of their in vivo efficacy on nude mice xenografted human hepatoma HepG2. The results showed that compounds 3 and 6 had considerable in vivo activity against HepG2, with tumor growth inhibition rates of 70% and 64% on day 21, respectively, and 56% and 55% on day 35, respectively, which are roughly comparable to capecitabine(74% and 59% on days 21 and 35, respectively).

引用

页码：78 / 83

页数：6

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