Table 1.
Ki values of the synthesized ANPs for APRT1 and anti-trypanosomal activity of their prodrugs.
| General structure (A = adenin-9-yl) | ANP R=O− |
APRT1 Ki [μM] |
Prodrug, R = 
|
T. brucei BSF EC50 (μM) |
Cytotoxicity of prodrug: NHDF/HeLaS3 viability (%)a |
|---|---|---|---|---|---|
|
3a | 10.1 ± 1.1 | 24a |
BSF427, HMI-11 6.16 ± 0.59 |
89/99 |
| BSF427, HMI-11adenine 6.36 ± 0.12 | |||||
|
3b | > 30 | 24b |
BSF427, HMI-11 6.36 ± 0.95 |
89/98 |
| BSF427, HMI-11adenine 6.16 ± 0.09 | |||||
|
4a | > 30 | – | – | – |
|
4b | > 30 | – | – | – |
|
9a | 4.92 ± 0.43 | – | – | – |
|
9b | > 30 | – | – | – |
|
9c | > 30 | – | – | – |
|
9d | 3.88 ± 0.29 | – | – | – |
|
9e | > 30 | – | – | – |
|
9f | > 30 | – | – | – |
|
9g | 3.07 ± 0.25 | 27 |
BSF427, HMI-11 2.26 ± 0.69 |
85/99 |
| BSF427, HMI-11adenine 3.21 ± 1.56 | |||||
|
APRT1OE, HMI-11 2.26 ± 0.08 | |||||
| APRT1OE, HMI-11adenine 0.81 ± 0.2 | |||||
|
17 | 21.3 ± 2.1 | 28 |
BSF427, HMI-11 0.99 ± 0.24 |
4/94 |
| BSF427,HMI-11adenine 0.86 ± 0.31 | |||||
|
APRT1OE, HMI-11 0.86 ± 0.08 | |||||
| APRT1OE, HMI-11adenine 0.83 ± 0.09 | |||||
|
20 | 27.7 ± 4.5 | 26 |
BSF427, HMI-11 1.55 ± 0.07 |
88/100 |
|
21 | > 30 | – | – | – |
|
22 | 5.15 ± 0.69 | 25 |
BSF427, HMI-11 3.7 ± 1.9 |
90/99 |