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. Author manuscript; available in PMC: 2020 May 27.
Published in final edited form as: J Med Chem. 2019 May 9;62(10):5217–5241. doi: 10.1021/acs.jmedchem.9b00532

Table 6.

Antiproliferative Activity of Selected Analogs in Cell Lines with Truncated APC

Cpd. IC50 ± (nM)a
CLipE
DLD-1 HT-29 CTRPA A1309b
6 63 ± 5.6 53 ± 2.3 122±6.5 6.68
22 4.8 ± 0.5 2±0.1 3.8 ± 0.7 6.86
29 3.2 ± 0.06 1.2 ± 0.07 6.9±0.8 7.02
30 3 ± 0.25 3 ± 0.05 2.8 ±0.03 7.04
32 4.5 ± 0.2 4±0.1 10.5 ± 0.3 7.94
33 2 ± 0.006 2 ± 0.004 0.7 ± 0.02 7.37
38 0.6 ± 0.02 0.5±0.1 0.8 ± 0.03 6.75
40 2.9 ± 0.34 2.2 ± 0.06 8.2±0.63 6.63
45 5 ± 0.07 4 ± 0.02 9.6 ± 0.3 5.37
46 3 ± 0.23 2.2±0.3 3.4 ± 0.7 6.25
47 0.03 ± 0.0001 0.9 ± 0.08 0.04 ± 0.002 8.32
48 2 ± 0.05 1.1 ± 0.04 3.2 ± 0.4 6.26
49 0.6 ± 0.01 0.45 ± 0.01 0.7 ± 0.05 6.79
51 0.96 ± 0.002 0.74 ± 0.03 1.2 ± 0.06 6.67
60 5 ± 0.06 6 ± 0.07 10.2 ± 0.8 5.81
61 2 ± 0.3 2 ± 0.07 1.6 ±0.3 6.36
81 1.6 ± 0.03 1.5 ± 0.03 3.4 ± 0.3 8.17
85 1.2 ± 0.03 0.8 ± 0.03 1.5 ±0.08 6.14
87 0.65 ± 0.002 0.34 ± 0.02 0.94 ±0.01 7.50
92 0.2 ± 0.03 0.12 ± 0.05 0.9±0.07 8.15
96 3 ± 0.04 2.1±0.07 3.4 ± 0.8 5.31
98 0.3 ± 0.002 0.2 ± 0.001 0.6 ± 0.003 6.69
108 3.5 ± 0.03 3 ± 0.2 4.3 ± 0.1 4.70
a

IC50 values represent the half maximal (50%) inhibitory concentration as determined in the CellTiter-Glo® (Promega) assay. Error represents SD (n = 3). All compounds were inactive when counter-screened against the HCT116 cell line with wild-type APC status (IC50 > 5 μM).

b

All compounds were inactive when counter-screened against the isogenic CTRPA cell line with wild-type APC status (IC50 > 5 μM).