Table 3. Antiproliferative activity of piperazinylquinoxalines (14–53).
IC50 (µM)a | ||||||
Cpd. | 2-substituenton quinoxaline | PC3 | A549 | HCT116 | HL60 | KB |
14 | 4-methylpiperazin-1-yl | 2.94 | 14.03 | 2.78 | 0.77 | 4.54 |
15 | 4-methylpiperazin-1-yl | 0.84 | 2.4 | 1.68 | 0.69 | 0.47 |
16 | 4-methylpiperazin-1-yl | 1.55 | 8.57 | 2.37 | 0.54 | 2.53 |
17 | 4-methylpiperazin-1-yl | 1.01 | 5.18 | 2.31 | 0.28 | 0.87 |
18 | 4-methylpiperazin-1-yl | 3.09 | 7.95 | 8.21 | 2.75 | 21.64 |
19 | piperazin-1-yl | 0.90 | 12.82 | 0.99 | 0.11 | 8.27 |
20 | piperazin-1-yl | 1.32 | 14.39 | 0.47 | 0.12 | 7.26 |
21 | piperazin-1-yl | 0.68 | 1.37 | 0.63 | 0.16 | 11.48 |
22 | piperazin-1-yl | 0.36 | 0.75 | 0.19 | 0.10 | 9.89 |
23 | piperazin-1-yl | 2.05 | 2.79 | 2.43 | 1.39 | 4.58 |
24 | 3-methylpiperazin-1-yl | 1.44 | 1.36 | 0.68 | 0.15 | 8.73 |
25 | 3-methylpiperazin-1-yl | 2.03 | 1.60 | 1.17 | 0.09 | 9.18 |
26 | 3-methylpiperazin-1-yl | 0.93 | 1.65 | 0.54 | 0.16 | 8.53 |
27 | 3-methylpiperazin-1-yl | 0.60 | 0.57 | 0.32 | 0.12 | 9.46 |
28 | 3-methylpiperazin-1-yl | 2.34 | 3.45 | 2.20 | 1.95 | 2.03 |
29 | 4-benzoylpiperazin-1-yl | 4.99 | 5.20 | 42.36 | 7.20 | 1.22 |
30 | 4-benzoylpiperazin-1-yl | 5.81 | 8.03 | 6.90 | 17.28 | 3.67 |
31 | 4-benzoylpiperazin-1-yl | 3.63 | 7.43 | 17.24 | 6.93 | 5.65 |
32 | 4-benzoylpiperazin-1-yl | 1.40 | 3.96 | 10.08 | 17.37 | 3.37 |
33 | 4-benzoylpiperazin-1-yl | 1.77 | 1.16 | 8.88 | 6.95 | 1.22 |
34 | 4-(4-chlorobenzoyl)piperazin-1-yl | 2.74 | 3.86 | 25.38 | 5.84 | 0.93 |
35 | 4-(4-chlorobenzoyl)piperazin-1-yl | 3.61 | 21.57 | 9.84 | 6.09 | 2.84 |
36 | 4-(4-chlorobenzoyl)piperazin-1-yl | 2.43 | >50 | 9.62 | 5.58 | 6.03 |
37 | 4-(4-chlorobenzoyl)piperazin-1-yl | 2.89 | >50 | 10.57 | 6.11 | 5.09 |
38 | 4-(4-chlorobenzoyl)piperazin-1-yl | 4.05 | 17.70 | 8.75 | 4.44 | 1.88 |
39 | 4-(methylsulfonyl)piperazin-1-yl | 1.07 | 2.37 | 1.21 | NTb | NTb |
40 | 4-(methylsulfonyl)piperazin-1-yl | 5.35 | 1.93 | 1.07 | NTb | NTb |
41 | 4-(methylsulfonyl)piperazin-1-yl | 2.21 | 1.32 | 0.55 | NTb | NTb |
42 | 4-(methylsulfonyl)piperazin-1-yl | 1.95 | 1.32 | 0.41 | NTb | NTb |
43 | 4-(methylsulfonyl)piperazin-1-yl | 3.30 | 1.26 | 0.33 | NTb | NTb |
44 | 4-tosylpiperazin-1-yl | 2.19 | 24.26 | 7.49 | 6.40 | 3.08 |
45 | 4-tosylpiperazin-1-yl | 3.48 | 49.47 | 1.92 | 9.28 | 2.68 |
46 | 4-tosylpiperazin-1-yl | 6.20 | >50 | 14.22 | 14.95 | 2.35 |
47 | 4-tosylpiperazin-1-yl | 4.89 | 19.51 | 5.07 | 10.27 | 2.73 |
48 | 4-tosylpiperazin-1-yl | 3.39 | 48.23 | 3.76 | 9.48 | 5.17 |
49 | 4-(3-morpholinopropyl)piperazin-1-yl | 5.12 | 0.73 | 0.65 | NTb | NTb |
50 | 4-(3-morpholinopropyl)piperazin-1-yl | 3.83 | 0.51 | 0.31 | NTb | NTb |
51 | 4-(3-morpholinopropyl)piperazin-1-yl | 9.30 | 2.10 | 2.59 | NTb | NTb |
52 | 4-(3-morpholinopropyl)piperazin-1-yl | 1.19 | 0.34 | 0.22 | NTb | NTb |
53 | 4-(3-morpholinopropyl)piperazin-1-yl | 4.80 | 1.12 | 0.93 | NTb | NTb |
LYc | – | 61.35 | 89.65 | 56.01 | 9.94 | 44.76 |
The mean value of at least two separate determinations.
NT: not tested.
LY: LY294002.