Table 1. a Activity of synthesized acyclic aza-C-nucleoside phosph(on)ates as inhibitors of Pf and human (Hs) HGXPRT.
| Pf HGXPRT Ki (nM) | Hs HGPRT Ki (nM) | Pf HGXPRT Ki (nM) | Hs HGPRT Ki (nM) | ||
|---|---|---|---|---|---|
| 19 | > 20,000 | > 10,000 | 61 | 1.2 ± 0.1 | 420 ± 10 > 10,000 |
| 20 | 1,900 ± 100 | > 10,000 | 65 | 87 ± 8 | |
| 4 | 10.6 ± 1.324 | 4,900 ± 30024 | 72 | 100 ± 11 | > 10,00 0 |
| 21 | 490 ± 35 | > 10,000 | 75 | 14,400 | > 10,000 |
| 22 | 8,600 ± 900 | > 10,000 | 80 | 19 ± 2 | > 10,000 |
| 24 | 27.6 ± 1.9 | > 10,000 | 81 | 9,400 | > 10,000 |
| 31 | 620 ± 61 | > 10,000 | 84 | 15,300 | > 10,000 |
| 32 | > 20,000 | 11,320 ± 1,300 | 87 | 2.4 ± 0.2 | > 10,000 |
| 44 | 9.1 ± 0.1 | > 10,000 | 88 | 14.3 ± 1.7 | > 10,000 |
| 45 | 490 ± 60 | > 10,000 | 90 | 650 ± 150 | > 10,000 |
| 53 | 0.65 ± 0.0424 | 380 ± 4024 | 95 | 980 ± 70 | > 10,000 |
| 57 | 23.4 ± 2.3 | 16,000 ± 1,000 |
a
The Ki values were determined from analyses assuming competitive inhibition as in ref. 24.