Table 1. List of starting materials employed and the types of poly-substituted purines synthesized. Half-inhibitory concentrations (IC50) against the protozoan parasite Trypanosoma brucei presented as mean ± SEM. n = 6.
entry | R1 | R2 | R3 | “A”% (R1, R2, R3) | “B”% (R2,R3) | IC50 (μM)a T.brucei |
---|---|---|---|---|---|---|
A1 | Me | Ph | iPr | 16% | traces | 69.2 ± 1.8 |
A2 | Et | Me | iPr | 29% | traces | 137.1 ± 6.9 |
A31 | Et | Me | Bu | 31% | traces | 51.8 ± 3.3 |
A4 | H | Me | iPr | 44% | - | 14.7 ± 0.6 |
A5 | H | Ph | iPr | 38% | - | 1 ± 0.1 |
B1 | Et | Ph | iPr | - | 40% | 52.1 ± 1 |
B2 | Et | Ph | tBu | - | 45% | 18.3 ± 0.5 |
B3 | Et | MeOPh | iPr | - | 28% | 42.7 ± 1 |
B4 | Et | MeOPh | tBu | - | 22% | 80.5 ± 3.5 |
B5 | iPr | H | iPr | - | 10% | 37.5 ± 1.5 |
B6 | iPr | Me | iPr | - | 10% | 32 ± 1.7 |
B7 | Ph | Me | iPr | - | 20% | 22.7 ± 1.4 |
B8 | Ph | Et | iPr | - | 27% | 4.8 ± 0.2 |
B9 | Ph | iPr | iPr | - | 22% | 12.6 ± 0.6 |
aCell viability was assessed by resazurin dye. Half-inhibitory concentration (IC50) values were calculated using GraphPad Prism5 Software and defined as the concentration of purine required to diminish fluorescence output by 50%. n = 6.