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. Author manuscript; available in PMC: 2011 Nov 15.
Published in final edited form as: Bioorg Med Chem Lett. 2010 Sep 21;20(22):6560–6564. doi: 10.1016/j.bmcl.2010.09.046

Table 1.

Effect of N-aryl maleimide ring substitution on GST-Bfl-1 inhibition

graphic file with name nihms-244783-t0004.jpg
Compound
#
R1 Bfl-1 FPa
IC50 (μM)
Bfl-1 TR-FRETa
IC50 (μM)
1 3,4-dichloro-phenyl 0.6±0.1 0.8±0.1
8 3,5-dichloro-phenyl 2.4±0.4 1.9±0.2
9 2,4-dichloro-phenyl 2.6±0.2 1.4±0.1
10 2,3-dichloro-phenyl 8.7±1.7 2.6±0.1
11 2,6-dichloro-3-methyl-phenyl 23.9±3.9 11.1±2.3
12 2-chloro-phenyl 3.3±0.3 1.0±0.1
13 3-chloro-phenyl 2.1±0.2 1.2±0.1
14 3-methyl-phenyl 12.6±2.3 10.8±0.9
15 3-nitro-phenyl 6.8±1.4 3.9±0.4
16 3-Chloro-pyridin-4yl 29±3.9 35.6±3.9
a

Data are the mean ± SEM.