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. 2015 Mar 16;5:9139. doi: 10.1038/srep09139

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.