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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 1b.

Effect of the R1 region (4-biphenyl substituents) on TGFβ inhibition.agraphic file with name nihms-419834-t0008.jpg

compd Y Z IC50 (μM) %inhibition (2.5 μM)
10 H H 1.49 ± 0.43 44 ± 5
13 H F 1.84 ± 0.35 59 ± 1
14 4”-CO2Me H 1.35 ± 0.16 78 ± 1
34 4”-Me H 0.86 ± 0.15 88 ± 2
35 4”-CF3 H 0.73 ± 0.41 91 ± 6
36 3”-Cl H 1.52 ± 0.18 73 ± 1
37 2”-Me H 0.89 ± 0.01 87 ± 2
38 2”-F H 2.06 ± 0.09 58 ± 1
a

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