COX-2-IN-1 is potent and slective COX-2 inhibitor with an IC50 of 3.9 μM.
COX-2-IN-1(compound 5f) is an inhibitor of COX-1 and COX-2 with IC50s of >100 and 3.9 μM, respctively. Comparison of 5b and COX-2-IN-1 shows that smaller halogen atom at 5th position on the indole ring enhances COX-2 enzyme inhibition activity, whereas the presence of a larger bromine atom at 6th position of the ring improves the inhibitory activity (5d, 5e and 5h) of the compound[1].
[1]. Reddy MV, et al. Design, synthesis, and biological evaluation of 1-(4-sulfamylphenyl)-3-trifluoromethyl-5-indolyl pyrazolines as cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) inhibitors. Bioorg Med Chem. 2008 Apr 1;16(7):3907-16.