Biological evaluation of 2-aryl-2-fluoropropionic acids as possible platforms for new medicinal agents.
Biological evaluation of 2-aryl-2-fluoropropionic acids as possible platforms for new medicinal agents.
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DOI：
10.1002/chin.200604215
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发表时间：
2005-08
影响因子：
1.7
通讯作者：
Y. Takéuchi;H. Fujisawa;Tomoya Fujiwara;M. Matsuura;Hirotsugu Komatsu;S. Ueno;T. Matsuzaki
中科院分区：
文献类型：
--
作者：
Y. Takéuchi;H. Fujisawa;Tomoya Fujiwara;M. Matsuura;Hirotsugu Komatsu;S. Ueno;T. Matsuzaki
我们研究了 2-芳基-2-氟丙酸 1a-e 的环氧合酶 (COX) 抑制和抗癌活性。这些氟化化合物对COX-1的抑制活性低于相应的非氟化化合物2a-e，但保留了对COX-2的抑制活性，导致COX-1/COX-2抑制的平衡发生改变，并且它们几乎没有表现出抗癌活性。在某些情况下，观察到 (S)- 和 (R)- 对映体之间的活性存在有趣的差异。
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.