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 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）.