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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 4.

Effect of the R4,5 region on TGFβ inhibition.agraphic file with name nihms-419834-t0019.jpg

compd R4 R5 IC50 (μM) %inhibition (2.5 μM)
10 Me Me 1.49 ± 0.43 44 ± 5
21 H Me 2.73 ± 0.75 48 ± 6
22 H Et 0.79 ± 0.15 92 ± 1
23 H nPr 0.53 ± 0.20 96 ± 2
24 H iPr 0.94 ± 0.44 83 ± 8
25 H iBu 0.59 ± 0.21 94 ± 2
26 H Ph 1.92 ± 0.20 61 ± 1
27 H 4-(N(Me)2)Ph 3.97 ± 0.94 40 ± 6
a

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