Biological evaluation of 2-aryl-2-fluoropropionic acids as possible platforms for new medicinal agents.
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.
Takeuchi
Yoshio
Y
Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University, Sugitani 2630, Toyama 930-0194, Japan. takeuchi@ms.toyama-mpu.ac.jp
Fujisawa
Hidehito
H
Fujiwara
Tomoya
T
Matsuura
Mamoru
M
Komatsu
Hirotsugu
H
Ueno
Satoshi
S
Matsuzaki
Takeshi
T
D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D011422:Propionates / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism
D000970:Antineoplastic Agents; D016861:Cyclooxygenase Inhibitors; D011422:Propionates; C029658:propionic acid