Skip to main content
. Author manuscript; available in PMC: 2015 Feb 18.
Published in final edited form as: J Med Chem. 2014 Feb 18;57(4):1188–1207. doi: 10.1021/jm401551n

Table 1.

graphic file with name nihms572303u2.jpg
compd X1 = X2 X3 X5, X6 X7 IC50 (μM) growth inhibitiona IC50 (μM) caspase-3,7 activationb
17a N -NH2 2 × -OCH3 methylpiperazine 0.90 ± 0.2 1.2 ± 0.4
17b N -NH2 2 × -OCH3 morpholine 12.5 ± 0.7 12.1 ± 2.5
17c N -NH2 2 × -OCH3 piperidine 17.1 ± 2.2 16.2 ± 0.5
20a N -NH2 2 × -OC2H5 methylpiperazine 0.89 ± 0.2 4.0 ± 0.0
20b N -NH2 2 × -OC2H5 morpholine 2.2 ± 1.2 10.5 ± 3.5
20c N -NH2 2 × -OC2H5 piperidine 4.5 ± 0.2 4.0 ± 2.0
27a N -H 2 × -OCH3 methylpiperazine 1.25 ± 0.7 4.0 ± 0.5
27b N -H 2 × -OCH3 morpholine 2.0 ± 0.5 7.2 ± 0.7
27c N -H 2 × -OCH3 piperidine 3.15 ± 1.5 12.4 ± 1.5
27d N -H 2 × -OCH3 pyrrolidine 46.1 ± 15.5 >100
28 N -H 2 × -OCH3 1-methylpiperazine 1-oxide >100 >100
30 N -H 2 × -OCH3 -OCH3 ND 7.5 ± 0.3
31 N -NH2 2 × -OCH3 -NH2 3.9 ± 1.4 4.5 ± 0.5
36a C -H 2 × -OCH3 methylpiperazine 7.8 ± 1.1 ND
37 C -H 2 × -OCH3 morpholine 46.5 ± 3.4 27.5 ± 2.5
42a N -H 2 × -CH3 methylpiperazine ND 6.0 ± 2.1
43 N -H 2 × -CH3 morpholine 14.4 ± 2.7 15.4 ± 0.7
44a N -NH2 2 × -OCH3 2-(2-(2-(2-(piperazin-1-yl)ethoxy)ethoxy) ethoxy) ethanol 3.8 ± 1.2 14.3 ± 1.5
45a N -NH2 -OCH3, -(OC2H4O)4H methylpiperazine 76.5 ± 21.5 100 ± 10.5
a

Inhibition of growth measured in Kasumi-1 acute myeloid leukemia cells. Values are the mean ± SEM.

b

Caspase-3,7 activation measured in MOLM13 acute myeloid leukemia cells. Values are the mean ± SEM.