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%.