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. Author manuscript; available in PMC: 2015 Jun 1.
Published in final edited form as: Bioorg Med Chem. 2014 Apr 16;22(11):2919–2938. doi: 10.1016/j.bmc.2014.04.014

Table 4.

The effect of varying the substitution pattern of the 1,3,4-substituted-pyrazole-4-carboxamide derivatives on their biological activities (N-methylation).

graphic file with name nihms617900t12.jpg
Cmpd R1 R2 FXR TR-FRET Binding GB FXR Cell Anta. GB FXR Cell Cyto
%Inh. IC50 %Inh. IC50 %Inh. IC50
8a (CH3)2CH 4-CH3-Ph 132.9±6.2 (40 µM) 489.4±21.2 nM 86.4±2.8 (40 µM) 16.16±0.28 µM 15.0±0.7 (40 µM) NA
8b graphic file with name nihms617900t13.jpg (CH3)2CH 80.3±5.2 (40 µM) 5.33±0.24 µM 2.4±0.1 (20 µM) NA 13.5±0.4 (40 µM) NA
8c graphic file with name nihms617900t14.jpg 3-CH3O-Ph 69.7±3.5 (40 µM) 3.81±0.20 µM 23.8±0.4 (40 µM) NA 19.7±0.4 (40 µM) NA