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. Author manuscript; available in PMC: 2012 Oct 1.
Published in final edited form as: Cancer Prev Res (Phila). 2011 Sep 7;4(10):1536–1545. doi: 10.1158/1940-6207.CAPR-11-0120

Table 1. Biochemical properties of fluorinated indomethacin and celecoxib derivatives.

The IC50's for inhibition of purified ovine COX-1, human COX-2, or COX-2 in lipopolysaccharide activated macrophage-like RAW246.7 cells.

Compound No. Structure Purified Enzyme IC50 (μM) RAW246.7 Cellsa IC50 (μM) COX-2
COX-1 COX-2
1 graphic file with name nihms323931t1.jpg > 4 0.14 0.68
2 graphic file with name nihms323931t2.jpg > 4 0.09 0.01
3 graphic file with name nihms323931t3.jpg > 4 0.26 0.16
4 graphic file with name nihms323931t4.jpg > 4 0.10 0.04
5 graphic file with name nihms323931t5.jpg > 4 0.16 0.24
6 graphic file with name nihms323931t6.jpg > 4 0.13 0.11
7 graphic file with name nihms323931t7.jpg > 4 0.16 0.08
8 graphic file with name nihms323931t8.jpg > 4 0.60 N.T.
9 graphic file with name nihms323931t9.jpg > 4 1.95 N.T.
10 graphic file with name nihms323931t10.jpg > 4 3.40 N.T.
11 graphic file with name nihms323931t11.jpg > 4 1.3 N.T.
Indomethacin graphic file with name nihms323931t12.jpg 0.05 0.75 0.01
Celecoxib graphic file with name nihms323931t13.jpg > 4 0.03 N.T.
a

Assays were conducted as described in Materials and Methods. Compounds that are poor inhibitors of COX-2 in the purified enzyme assay were not tested (N.T.) in intact cells.