Synthesis and Antitumor Activity of Capecitabine Derivatives

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 xenografte...

Full description

Saved in:
Bibliographic Details
Published in:Chemical research in Chinese universities 2015-02, Vol.31 (1), p.78-83
Main Authors: Jia, Xuedong, Liu, Xiujun, Wang, Jian, Wang, Minghua, Guo, Huiyuan, Liu, Mingliang
Format: Article
Language:English
Subjects:
Analytical Chemistry
Chemistry
Chemistry and Materials Science
Chemistry/Food Science
HepG2
Inorganic Chemistry
Organic Chemistry
Physical Chemistry
体内活性
体外抗肿瘤活性
化合物
合成
异种移植
生长抑制率
衍生物
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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）.
ISSN:1005-9040
2210-3171
DOI:10.1007/s40242-015-4282-4