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. Author manuscript; available in PMC: 2013 Sep 1.
Published in final edited form as: Biochimie. 2012 May 29;94(9):1974–1981. doi: 10.1016/j.biochi.2012.05.020

Table 1.

Structure-activity relationships for binding affinity at TDP-43 and stimulation of caspase-7 mediated cleavage of TDP-43.

graphic file with name nihms386548u1.jpg
IC50 (μM)a TDP-43 binding Stimulation of caspase-7 cleavage of TDP-43 (%)b
C# R1 R2 10 μM 3.2 μM 1.0 μM
2 graphic file with name nihms386548t1.jpg —OCH3 5.6 (2.7–11) 123 ± 20 56 ± 22 10 ± 9
3 —CH2CH3 20 (8.0–50) 17 ± 5 ND ND
1 graphic file with name nihms386548t2.jpg —OCH3 1.1 (0.55–2.2) 117 ± 11 84 ± 24 15 ± 7
4 —CH2CH3 3.3 (1.3–8.4) 26 ± 8 ND ND
5 graphic file with name nihms386548t3.jpg —OCH3 4.0 (2.1–7.6) 124 ± 18 129 ± 24 14 ± 5
6 —CH2CH3 7.6 (4.9–12) 24 ± 9 ND ND
7 graphic file with name nihms386548t4.jpg —OCH3 8.9 (5.4–15) 4 ± 5 ND ND
8 graphic file with name nihms386548t5.jpg —OCH3 24 (7.8–74) 9 ± 4 ND ND
9 graphic file with name nihms386548t6.jpg —H >100 c4 ± 2 ND ND
a

IC50 values are the geometric mean and 95% confidence intervals of at least three determinations.

b

Values are the mean ± S.E.M. of three determinations and represent relative stimulation where 0% and 100% are equal to the intensity of CTF35 in the absence and presence of 10 μM T798, respectively.

c

Stimulation value at 32 μM compound.

ND. Not determined.