Synthesis and Antitumor Activity of Capecitabine Derivatives

doi:10.1007/s40242-015-4282-4

高等学校化学研究 ›› 2015, Vol. 31 ›› Issue (1): 78-83.doi: 10.1007/s40242-015-4282-4

Synthesis and Antitumor Activity of Capecitabine Derivatives

JIA Xuedong^1,2, LIU Xiujun¹, WANG Jian³, WANG Minghua¹, GUO Huiyuan¹, LIU Mingliang¹

1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, P. R. China;
2. The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, P. R. China;
3. No.5 Hospital of Harbin, Harbin 150040, P. R. China

收稿日期:2014-07-25 修回日期:2014-09-11 出版日期:2015-02-01 发布日期:2014-10-20
通讯作者: LIU Mingliang, E-mail:lmllyx@126.com;LIU Xiujun, E-mail:liuxiujun2000@163.com E-mail:lmllyx@126.com;liuxiujun2000@163.com
基金资助:
Supported by the National S&T Major Special Project on Major New Drug Innovations of China(Nos.2012ZX09301002-001-017/023, 2014ZX09507009-003) and the National Natural Science Foundation of China(No.81373267-003).

Synthesis and Antitumor Activity of Capecitabine Derivatives

JIA Xuedong^1,2, LIU Xiujun¹, WANG Jian³, WANG Minghua¹, GUO Huiyuan¹, LIU Mingliang¹

1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, P. R. China;
2. The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, P. R. China;
3. No.5 Hospital of Harbin, Harbin 150040, P. R. China

Received:2014-07-25 Revised:2014-09-11 Online:2015-02-01 Published:2014-10-20
Contact: LIU Mingliang, E-mail:lmllyx@126.com;LIU Xiujun, E-mail:liuxiujun2000@163.com E-mail:lmllyx@126.com;liuxiujun2000@163.com
Supported by:
Supported by the National S&T Major Special Project on Major New Drug Innovations of China(Nos.2012ZX09301002-001-017/023, 2014ZX09507009-003) and the National Natural Science Foundation of China(No.81373267-003).

摘要/Abstract

摘要：

A series of capecitabine derivatives with a Boc group at the N⁴-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).

关键词: Capecitabine, Derivative, Antitumor activity

Abstract:

Key words: Capecitabine, Derivative, Antitumor activity

JIA Xuedong, LIU Xiujun, WANG Jian, WANG Minghua, GUO Huiyuan, LIU Mingliang. Synthesis and Antitumor Activity of Capecitabine Derivatives[J]. 高等学校化学研究, 2015, 31(1): 78-83.

JIA Xuedong, LIU Xiujun, WANG Jian, WANG Minghua, GUO Huiyuan, LIU Mingliang. Synthesis and Antitumor Activity of Capecitabine Derivatives[J]. Chemical Research in Chinese Universities, 2015, 31(1): 78-83.

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Synthesis and Antitumor Activity of Capecitabine Derivatives

Synthesis and Antitumor Activity of Capecitabine Derivatives

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