Skip to main content
. 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 2. Enzymatic results for compounds 27-47.

graphic file with name nihms746040u3.jpg
No. R R1 R2 HsRcel Percent Activity Remaining (10 μM)a HsRcel IC50 (μM)b
27 H H H 17 ±0.4 4.9±1.1
28 p-t-butyl H H 38 ±0.47 5.0±1.1
29 p-CO2H H H 19 ±2.4 4.2±1.1
30 m-CO2H H H 23 ±5.5 5.3 ±1.1
31 p-CO2H Br H 23 ±1.1 3.9 ±1.0
32 CO2Me H graphic file with name nihms746040t2.jpg 65 ±2.1 nd
33 H H graphic file with name nihms746040t3.jpg 27 ±3.2 5.4 ±1.1
34 H H graphic file with name nihms746040t4.jpg 59 ±0.65 nd
35 H H graphic file with name nihms746040t5.jpg 51 ±2.9 nd
36 H H graphic file with name nihms746040t6.jpg 83 ±6.9 nd
37 H H graphic file with name nihms746040t7.jpg 83 ± 0.1 nd
38 H H graphic file with name nihms746040t8.jpg 77 ± 3.9 nd
39 H H graphic file with name nihms746040t9.jpg 75 ± 2.9 nd
40 H H graphic file with name nihms746040t10.jpg 68 ± 0.7 nd
41 H H graphic file with name nihms746040t11.jpg 73 ± 3.5 nd
42 H H graphic file with name nihms746040t12.jpg 51 ± 2.0 nd
43 H H graphic file with name nihms746040t13.jpg 82 ± 0.3 nd
44 H H graphic file with name nihms746040t14.jpg 77 ± 2.8 nd
45 H - - 45 ±0.32 9.4 ±1.1
46 CO2H - - 21 ±2.4 3.8 ±1.1
47 - - - 63 ±0.08 nd
a

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

b

nd = Not determined