Author: Jing Wang, Mei-Juan Zou, Lei Chen, Yi-Ling Sheng, Xiao-Mian Zhou and Xiang-Rong Zhang
Publishing Date: 2016
Volume 29 Issue 6
The objective of this work is to synthesize indolacin-5-fluorouracil-1-ylmethyl ester and the structure was confirmed by means of UV, IR, 1H-NMR, 13C-NMR and mass spectrometry. The physicochemical parameters of melting point, solubility, apparent partition coefficient were investigated. S180 sarcoma, H22 hapatitic cancer and Lewistransplanted mice were used to evaluate the anti-tumor activity of indolacini-5-fluorouracil-1-ylmethyl ester compared with 5-fluorouracil in vivo. Anti-inflammatory and analgesic activities were evaluated in mice. The inhibitory ratio of indolacini- 5-fluorouracil-1-ylmethyl ester is comparative to that of 5-fluorouracil. This study indicates that 5- fluorouracil-1-ylmethyl ester may represent a new anticancer predrug of 5-fluorouracil to produce a combined effect of indolacin and 5-fluorouracil for cancer therapy.
KEYWORDS: 5-Fluorouracil, Indolacini-5-fluorouracil-1-ylmethyl ester, Anti-tumor; Anti-inflammatory; Analgesic activity; LD50 values