Table 3. Azapurine derivatives.
| Compound | Scaffold | CRK3:CYC6IC50 (µM) | IC50 against WT promastigote L. major (µM) | IC50 against WT amastigote L. major (µM) |
| 13 | A | 15.9 | >50 | ND |
| 14 | A | >50 | ND | ND |
| 15 | A | >50 | ND | ND |
| 16 | A | >50 | ND | ND |
| 17 | A | 39.1 | 7.4 | 5–15 |
| 18 | A | >50 | ND | ND |
| 19 | A | >50 | 5–50 | ND |
| 20 | A | >50 | ND | ND |
| 21 | A | >50 | ND | ND |
| 22 | B | >50 | ND | ND |
| 23 | B | >50 | ND | ND |
| 24 | A | >50 | ND | ND |
| 25 | B | >50 | ND | ND |
| 26 | B1 | >50 | ND | ND |
| 27 | A | 30.3 | 28.7 | 15–30 |
| 28 | A | >50 | 8.3 | 5–15 |
| 29 | B | >100 | 38.7 | Activity at 25 µM |
| 30 | B | >100 | 3.8 | Activity at 10 µM |
| 31 | B | >20 | 40 | Activity at 25 µM |
| 32 | B | >100 | >50 | >25 |
| 33 | A | 47.6 | >50 | >50 |
| 34 | A | >50 | 8.3 | 5–15 |
| 35 | A | >50 | >50 | >50 |
1
Compound 26 contains a 4-bromo substitution on the benzyl moiety of scaffold B (See Table S3 in Supporting Information Text S1 for compound structures). ND, not determined.