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. 2012 Jun 24;287(36):30444–30454. doi: 10.1074/jbc.M112.378091

TABLE 1.

Effect of natural pyrimidine and purine derivatives on the cytostatic activity of 3F-3DUrd and other antimetabolite drugs in CEM cell culture

Addition of natural DNA/RNA precursors IC50a
3F-3DUrd 3-DUrd Pyrazofurin 6-Aza-Urd K-oxonate A77 1726
μm
As such 19 ± 8.6 7.4 ± 3.1 0.24 ± 0.09 0.63 ± 0.28 204 ± 43 47 ± 41
+ Urd 500 μm >250 >250 >250 >250 >250 >250
+ Urd 100 μm >250 >250 >250 >250 >250 >250
+ Cyd 500 μm >250 >250 123 ± 121 >250 >250 >250
+ Cyd 100 μm >250 >250 99 ± 85 >250 >250 >250
+ Orotic acid 500 μm 13 ± 8.5 ≥27 0.24 ± 0.15 0.62 ± 0.30 >250 >250
+ Orotic acid 100 μm 10 ± 8.6 12 ± 5.8 0.26 ± 0.17 0.53 ± 0.25 ≥250 153
+ Orotidine 100 μm 6.8 ± 2.7 17 ± 10.3 0.079 ± 0.01 0.37 ± 0.17 149 ± 47 132
+ dThd 10 μm 11 ± 1.4 9 ± 4.0 0.20 ± 0.01 0.69 ± 0.06 82 ± 9.9 32 ± 6.1
+ dThd 5 μm 19 ± 8.6 9.6 ± 0.64 0.18 ± 0.11 0.75 ± 0.17 121 ± 82 61 ± 45
+ Hpx 100 μm 0.79 ± 0.44 3.55 ± 0.29 0.013 ± 0.007 0.045 ± 0.002 13 ± 2.3 114
+ Hpx 20 μm 2.2 ± 0.50 4.31 ± 0.88 0.12 ± 0.009 0.15 ± 0.01 105 ± 80 110
+ Gua 100 μm 4.9 ± 2.8 0.89 ± 0.16 0.17 ± 0.07 0.15 ± 0.07 42 ± 6.0 >50
+ Gua 20 μm 9.3 ± 0.47 10 ± 2.4 0.25 ± 0.13 0.54 ± 0.13 ≥250 106
+ Ado 500 μm 0.31 ± 0.13 2.0 ± 1.5 0.026 ± 0.015 0.031 ± 0.008 12 ± 2.1 18 ± 13
+ Ado 100 μm 0.87 ± 0.02 2.9 ± 0.69 0.082 ± 0.014 0.089 ± 0.012 76 ± 16 62 ± 48
+ Ade 500 μm 0.25 ± 0.18 2.3 ± 1.9 0.011 ± 0 0.013 ± 0 6.2 ± 1.1 31 13
+ Ade 100 μm 0.53 ± 0.33 4.0 ± 0.95 0.020 ± 0.005 0.031 ± 0.003 19 ± 13 31 ± 10
+ Ade 20 μm 3.2 ± 2.9 4.2 ± 2.4 0.14 ± 0.07 0.22 ± 0.09 150 ± 141 22.4
+ Guo 20 μm 16 ± 11 3.3 ± 3.1 0.29 ± 0.01 0.32 ± 0.22 ≥208 117
+ Ino 100 μm 1.3 ± 0.19 3.3 ± 0.0 0.031 ± 0.005 0.054 ± 0.021 29 ± 11 105
+ Ino 20 μm 3.5 ± 0.47 3.3 ± 0.05 0.11 ± 0 0.22 ± 0.007 110 ± 9.9 126 ± 9.9

a 50% Inhibitory concentration or compound concentration required to inhibit CEM cell proliferation by 50%.