Synthesis and Biological Evaluation of Licofelone Derivatives as Anticancer and Anti-inflammatory Agents

Title: Synthesis and Biological Evaluation of Licofelone Derivatives as Anticancer and Anti-inflammatory Agents

Volume: 8 Issue: 10

Author(s): Wukun Liu, Jinpei Zhou, Huibin Zhang, Hai Qian, Jiahan Yin, Kerstin Bensdorf and Ronald Gust

Affiliation:

Keywords: Anti-inflammatory activity, COX inhibition, Cytotoxicity, Licofelone, Synthesis, Anticancer, Non-steroidal anti-inflammatory drugs (NSAIDs), adenomatous polyposis, Column chromatography (CC), methylbenzoates, L-glutamine, DMEM, ELISA, ibuprofen, ANOVA, antimalaria

Abstract: Two C5-substituted licofelone derivatives were developed and investigated for cytotoxicity against mammary (MCF-7 and MDA-MB 231) as well as colon carcinoma (HT-29) cancer cells. Both compounds were at least 2-fold more active than 5-fluorouracil (5-FU) and licofelone against mammary carcinoma cells. At HT-29 cells, they were less active, but nevertheless distinctly as active as 5-FU and still 2-fold more active than licofelone. However, variation of the C5- carboxylic group results in an occasionally remarkable decrease of anti-inflammatory potency in in vitro and in vivo.

Cite this article as:

Liu Wukun, Zhou Jinpei, Zhang Huibin, Qian Hai, Yin Jiahan, Bensdorf Kerstin and Gust Ronald, Synthesis and Biological Evaluation of Licofelone Derivatives as Anticancer and Anti-inflammatory Agents, Letters in Drug Design & Discovery 2011; 8 (10) . https://dx.doi.org/10.2174/157018011797655223