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. Author manuscript; available in PMC: 2018 May 11.
Published in final edited form as: J Med Chem. 2017 Apr 25;60(9):3979–4001. doi: 10.1021/acs.jmedchem.7b00271

Table 2.

Structure-Activity Relationship for 6-Pyridyl Substituent

graphic file with name nihms898386u3.jpg
Compound R/Inhibitor IC50 (nM) PGE2 increase at Aq. Solubility (μg/mL)b
20 nMa 2.5 μMa
1 2-Thiophene 2.2 1.9 2.7 0.3
12g 2-Thiazole 1.4 1.7 2.5 1.1
12h 2-oxazole 1.4 1.9 2.4 2.8
12i 2-(N-Me-imidazole) 6.7 1.4 2.6 1.9
38a graphic file with name nihms898386t1.jpg 136
38b graphic file with name nihms898386t2.jpg 151
a

Fold-increase in PGE2 levels in A549 cell culture media relative to DMSO. Data color-coded to indicate more active (blue), less active (red) or equally active (white) as compound 1.

b

pH 7 citrate buffer, 0.1 M.