Biological Evaluation of 2-Aryl-2-fluoropropionic Acids as Possible Platforms for New Medicinal Agents

Yoshio Takeuchi; Hidehito Fujisawa; Tomoya Fujiwara; Mamoru Matsuura; Hirotsugu Komatsu; Satoshi Ueno; Takeshi Matsuzaki

doi:10.1248/cpb.53.1062

Notes

Biological Evaluation of 2-Aryl-2-fluoropropionic Acids as Possible Platforms for New Medicinal Agents

Yoshio Takeuchi, Hidehito Fujisawa, Tomoya Fujiwara, Mamoru Matsuura, Hirotsugu Komatsu, Satoshi Ueno, Takeshi Matsuzaki

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Keywords: 2-aryl-2-fluoropropionic acid, non-steroidal anti-inflammatory drug, epimerization, chiral fluorinated structure

JOURNAL FREE ACCESS

2005 Volume 53 Issue 8 Pages 1062-1064

DOI https://doi.org/10.1248/cpb.53.1062

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Abstract

We investigated the cyclooxygenase (COX) inhibitory and anticancer activities of 2-aryl-2-fluoropropionic acids 1a—e. These fluorinated compounds showed lower inhibitory activity toward COX-1 than the corresponding non-fluorinated compounds 2a—e with retained inhibitory activity against COX-2 resulting in modification of the balance of COX-1/COX-2 inhibitions, and they showed little anticancer activity. Interesting differences of the activities between (S)- and (R)-enantiomers were observed in some cases.

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