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

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

Journal Name: Letters in Drug Design & Discovery

Volume 8 , Issue 10 , 2011

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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.

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

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Article Details

Year: 2011
Page: [911 - 917]
Pages: 7
DOI: 10.2174/157018011797655223
Price: $65

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