Table 1.
Enzymatic CpCDPK1, TgCDPK1, SRC inhibition (IC50), Toxicity (CC50) against CRL-8155 and HepG2, and C. parvum cellular assay (EC50) results for pyrazolopyrimidine (PP) compounds (6-12).
 |
|||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| BKI | Entry | R2 | R1 | IC50 (μM) | Toxicity CC50 (μM) | EC50 (μM) | Solubility (μM) | ||||
| CpCDPK1 | TgCDPK1 | SRC | CRL-8155 | HEPG2 | C. parvum | pH 2.0 | pH 6.5 | ||||
| 1561 | 6 |  |
 |
0.0032 | 0.0020 | >10.0 | >40.0 | >40.0 | 0.464 | >100.0 | 87.1 |
| 1553 | 7 |  |
 |
0.0021 | 0.0010 | >10.0 | >40.0 | >40.0 | 1.63 | >95.0 | 50.0 |
| 1829 | 8 |  |
 |
0.019 | 0.025 | >10.0 | >80.0 | >40.0 | 0.882 | >100.0 | 98.7 |
| 1547 | 9 |  |
 |
0.0030 | 0.0033 | >10.0 | >80.0 | >80.0 | 5.89 | >100.0 | 88.0 |
| 1830 | 10 |  |
 |
0.0040 | 0.058 | >10.0 | >80.0 | >80.0 | 0.286 | 95.1 | 81.0 |
| 1676 | 11 |  |
 |
1.33 | 1.66 | >10.0 | >80.0 | >80.0 | 5.87 | 99.6 | 52.9 |
| 1677 | 12 |  |
 |
0.62 | 0.042 | >10.0 | >80.0 | >80.0 | >20.0 | >100.0 | >100.0 |