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. Author manuscript; available in PMC: 2017 Jan 15.
Published in final edited form as: Bioorg Med Chem. 2015 Nov 30;24(2):160–178. doi: 10.1016/j.bmc.2015.11.043

Table 3. Enzymatic results for compounds 48-58.

graphic file with name nihms746040u4.jpg
No. R R1 R2 HsRcel% Activity Remaining (10 μM)a HsRcel IC50 (μM)b
48 CO2Et H H 82 ±4.4 nd
49 CO2Et Br H 79 ± 3.4 nd
50 CO2Et Br Br 83 ± 7.6 nd
51 CO2H H H 90 ± 3.6 nd
52 CO2H Br H 86 ± 0.2 nd
53 CO2H Br Br 83 ± 2.6 nd
54 Ph H H 78 ± 1.0 nd
55 Ph Br H 78 ± 2.5 nd
56 Ph Br Br 80 ± 4.8 nd
57 graphic file with name nihms746040t15.jpg H H 89 ± 3.5 nd
58 graphic file with name nihms746040t16.jpg H H 72 ± 2.2 nd
a

The % activity remaining values are the averages of replicates from one assay in the presence of inhibitor.

b

nd = Not determined