Table 2. Structures and associated in vitro results for additional compounds with 1,3-dihydro-imidazol-2-one linker.
| ||||||
| Compound number | R1 | R2 | R3 | T. brucei a EC50 (nM) | CRL-8155 c CC50 (nM) | HepG2 d CC50 (nM) |
| 17 |
|
Cl | Cl | 3.0 ± 0.5 (n = 2) | >50 000 | >50 000 |
| 18 |
|
F | Cl | 5.9 ± 2.3 (n = 2) | 33 300 | >50 000 |
| 19 |
|
Cl | Cl | 1.8 < 0.9 b | 37 800 | 26 400 |
| 20 |
|
F | Cl | 5.1 ± 0.8 (n = 3) | >50 000 | >50 000 |
| 21 |
|
F | Cl | 2.3 ± 1.3 (n = 2) | >50 000 | >50 000 |
| 22 |
|
F | Cl | 16 ± 5 (n = 3) | 30 400 | 33 200 |
| 23 |
|
F | Cl | 5.8 ± 2.3 (n = 2) | >50 000 | >50 000 |
| 24 |
|
F | Cl | 3.0 ± 1.8 (n = 2) | >50 000 | >50 000 |
| 25 |
|
F | Cl | 4.6 ± 2.0 (n = 2) | >50 000 | >50 000 |
| 26 |
|
Cl | OMe | 1.0 ± 0.2 (n = 9) | >50 000 | >50 000 |
| 27 |
|
F | OMe | 1.8 ± 0.4 (n = 2) | >50 000 | >50 000 |
| 28 |
|
Cl | OMe | 3.6 ± 2.2 (n = 2) | >50 000 | >50 000 |
| 29 |
|
F | OMe | 4.6 ± 1.7 (n = 2) | >50 000 | >50 000 |
aControl for T brucei EC50 assay average ± SEM: pentamidine (2.0 ± 0.3 nM; n = 24).
bTwo values, unable to average.
cControl for CRL-8155 CC50 assay average ± SEM: quinacrine (5.1 ± 1.0 μM; n = 7).
dControl for HepG2 CC50 assay average ± SEM: quinacrine (9.1 ± 0.8 μM; n = 7).