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. 2012 Aug 14;7(8):e43171. doi: 10.1371/journal.pone.0043171

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
a

The mean value of at least two separate determinations.

b

NT: not tested.

c

LY: LY294002.