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. 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 1a.

Effect of the R1 region (4'-substituents) on TGFβ inhibition.agraphic file with name nihms-419834-t0001.jpg

compd R1 R2 R3 IC50 (μM) %inhibition (2.5 μM)
7 F Me Me >10 4 ± 2
8 H Me Me >10 6 ± 4
9 tBu Me Me 0.56 ± 0.01 79 ± 3
32 graphic file with name nihms-419834-t0002.jpg Me Me 0.59 ± 0.04 94 ± 1
10 graphic file with name nihms-419834-t0003.jpg Me Me 1.49 ± 0.43 44 ± 5
1 graphic file with name nihms-419834-t0004.jpg Et Me 0.85 ± 0.30 83 ± 8
11 b graphic file with name nihms-419834-t0005.jpg Me Me 8.80 18
12 graphic file with name nihms-419834-t0006.jpg Et Et 3.57 ± 0.11 41 ± 2
33 graphic file with name nihms-419834-t0007.jpg Me Me 4.05 ± 1.19 41 ± 6
a

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

b

For this compound a single experiment was done.