Synthesis, physicochemical characterization and pharmacological investigation of indolacin-5-fluorouracil-1-ylmethyl ester. | [Pakistan Journal of Pharmaceutical Sciences • 2016]

Author(s):

1. Jing Wang: School of Pharmacy, Shenyang Pharmaceutical University,103 Wenhua Road, Shenyang,China

2. Mei-Juan Zou: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, China

3. Lei Chen: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, China

4. Yi-Ling Sheng: School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Wenhua Road, Shenyang, China

5. Xiao-Mian Zhou: School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Wenhua Road, Shenyang, China

6. Xiang-Rong Zhang: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, China

Abstract:

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 5fluorouracil-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.

Page(s): 1997-2004

DOI: DOI not available

Published: Journal: Pakistan Journal of Pharmaceutical Sciences, Volume: 29, Issue: 6, Year: 2016

Keywords:

Antiinflammatory , analgesic activity , 5fluorouracil , Antitumor , Indolacini5fluorouracil1ylmethyl ester , LD50 values

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