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. Author manuscript; available in PMC: 2018 Oct 15.
Published in final edited form as: Bioorg Med Chem Lett. 2017 Sep 13;27(20):4614–4621. doi: 10.1016/j.bmcl.2017.09.022

Table 1.

Screening data for control 1 and basic acyclic amides 2–37.

Ar Cmpd R1 & R2 CC50 (μM)
HT29 PC3 MDA-MB-231
graphic file with name nihms907144t1.jpg 1 R1 = H, R2 = -CH2CH2N(CH3)2 0.65±0.03 3.12±0.15 2.67±0.08
2 R1 = H, R2 = -CH2CH2CH2N(CH3)2 2.46±0.14 6.99±0.19 5.18±0.46
3 R1 = H, R2 = -CH2CH2N(CH2CH3)2 1.54±0.05 5.45±0.35 4.20±0.17
4 R1 = H, R2 = -CH2CH2CH2N(CH2CH3)2 1.53±3.33 4.33±0.22 3.19±0.08
5 R1 = CH3, R2 = -CH2CH2N(CH3)2 1.83±0.04 5.63±0.26 3.98±0.45
6 R1 = CH3, R2 = -CH2CH2CH2N(CH3)2 2.18±0.03 6.98±0.27 5.41±0.42
7 R1 = CH2CH3, R2 = -CH2CH2N(CH2CH3)2 1.83±0.04 6.21±0.44 5.22±0.20
8 R1 = CH3, R2 = -CH2CH2N(CH2CH3)2 1.49±0.02 5.65±0.26 3.77±0.35
9 R1 = CH2CH3, R2 = -CH2CH2N(CH3)2 1.36±0.05 5.07±0.31 3.96±1.46
10 R1 = CH3, R2 = -CH2CH2N(CH3)H 2.80±0.07 6.75±0.24 5.84±0.35
11 R1 = CH3, R2 = -CH2CH2CH2N(CH3)H 2.90±0.05 7.65±0.29 7.66±0.49
12 R1 = CH2CH3, R2 = -CH2CH2N(CH2CH3)H 2.54±0.10 6.56±0.43 6.65±0.22
13 R1 = CH2CH3, R2 = -CH2CH2CH2N(CH2CH3)H 1.38±0.05 3.92±0.29 3.03±0.19
14 R1 = CH(CH3)2, R2 = -CH2CH2CH2N(CH(CH3)2)H 2.30±0.07 4.90±0.23 3.92±0.39

graphic file with name nihms907144t2.jpg 15 R1 = H, R2 = -CH2CH2CH2N(CH3)2 33.27±2.92 >50.00 >50.00
16 R1 = H, R2 = -CH2CH2N(CH2CH3)2 19.78±0.77 >50.00 >50.00
17 R1 = H, R2 = -CH2CH2CH2N(CH2CH3)2 27.12±2.0 >50.00 >50.00
18 R1 = CH3, R2 = -CH2CH2CH2N(CH3)2 38.92±7.98 >50.00 >50.00
19 R1 = CH2CH3, R2 = -CH2CH2N(CH2CH3)2 18.40±0.78 >50.00 >50.00
20 R1 = CH3, R2 = -CH2CH2N(CH2CH3)2 23.97±1.51 >50.00 >50.00
21 R1 = CH2CH3, R2 = -CH2CH2N(CH3)2 18.15±0.94 >50.00 >50.00
22 R1 = CH3, R2 = -CH2CH2N(CH3)H 34.53±2.45 >50.00 >50.00
23 R1 = CH3, R2 = -CH2CH2CH2N(CH3)H >50.00 >50.00 >50.00
24 R1 = CH2CH3, R2 = -CH2CH2N(CH2CH3)H 18.18±1.40 >50.00 >50.00
25 R1 = CH2CH3, R2 = -CH2CH2CH2N(CH2CH3)H 17.48±1.14 >50.00 >50.00
26 R1 = CH(CH3)2, R2 = -CH2CH2CH2N(CH(CH3)2)H 16.28±0.97 48.28±8.05 >50.00

graphic file with name nihms907144t3.jpg 27 R1 = H, R2 = -CH2CH2N(CH3)2 6.22±0.44 18.27±1.34 15.05±0.88
28 R1 = H, R2 = -CH2CH2CH2N(CH3)2 6.08±0.30 13.03±0.74 10.79±0.45
29 R1 = H, R2 = -CH2CH2N(CH2CH3)2 5.42±0.38 13.88±0.78 12.26±0.34
30 R1 = CH3, R2 = -CH2CH2N(CH3)2 4.68±0.23 11.44±0.52 10.78±0.65
31 R1 = CH3, R2 = -CH2CH2N(CH3)H 8.05±0.31 23.06±1.31 16.96±1.04

graphic file with name nihms907144t4.jpg 32 R1 = H, R2 = -CH2CH2N(CH3)2 1.57±0.07 4.88±0.53 3.63±0.27
33 R1 = H, R2 = -CH2CH2CH2N(CH3)2 1.05±0.05 3.25±0.13 1.93±0.13
34 R1 = H, R2 = -CH2CH2N(CH2CH3)2 1.12±0.05 4.48±0.32 3.54±0.24
35 R1 = CH3, R2 = -CH2CH2N(CH3)2 2.02±0.06 5.88±0.32 3.80±0.51

graphic file with name nihms907144t5.jpg 36 R1 = H, R2 = -CH2CH2N(CH3)2 6.89±0.58 28.90±2.05 18.06±1.07

graphic file with name nihms907144t6.jpg 37 R1 = H, R2 = -CH2CH2N(CH3)2 12.67±0.73 >50.00 37.46±3.45