Table 1.
Screening data for control 1 and basic acyclic amides 2–37.
Ar | Cmpd | R1 & R2 | CC50 (μM)
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HT29 | PC3 | MDA-MB-231 | |||
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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 | |
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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 | |
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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 | |
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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 | |
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36 | R1 = H, R2 = -CH2CH2N(CH3)2 | 6.89±0.58 | 28.90±2.05 | 18.06±1.07 |
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37 | R1 = H, R2 = -CH2CH2N(CH3)2 | 12.67±0.73 | >50.00 | 37.46±3.45 |