Skip to main content
. Author manuscript; available in PMC: 2013 Nov 26.
Published in final edited form as: J Med Chem. 2012 Nov 6;55(22):9946–9957. doi: 10.1021/jm301144g

Table 2.

Effect of the R2 region (carboxylic esters and amides) on TGFβ inhibition.agraphic file with name nihms-419834-t0015.jpg

compd R2 IC50 (μM) %inhibition (2.5 μM)
44 OH >10 21 ± 11
10 OMe 1.49 ± 0.43 44 ± 5
1 OEt 0.85 ± 0.30 83 ± 8
15 OCH2CF3 0.76 ± 0.22 85 ± 4
16 OiBu 0.53 ± 0.09 87 ± 1
17 OiPentyl 1.46 ± 0.43 71 ± 4
18 graphic file with name nihms-419834-t0016.jpg 0.83 ± 0.40 72 ± 8
19 graphic file with name nihms-419834-t0017.jpg 4.06 ± 1.03 40 ± 1
a

Data represent means ± SD of n = 2–4 independent experiments.