Table 1.
Inhibitory activity of compound library Tritrichomonas foetus and cytotoxicity against human prostate (PC-3) cancer cell line.
| Compound | R | R1 | Average % inhibition at 50 μM (Tritrichomonas foetus) | Cytotoxicity% inhibition |
||
|---|---|---|---|---|---|---|
| 0.2 μM | 2 μM | 20 μM | ||||
| 3a | H | Piperidine | 18.2 | 6.0 | 4.0 | 7.0 |
| 3b | H | Pyrrolidine | 10.6 | 7.0 | 7.0 | 3.0 |
| 3c | H | Morpholine | 9.1 | 13.4 | 11.6 | 8.7 |
| 3d | H | N,N-Diethylamine | 22.7 | 8.0 | 4.6 | 8.0 |
| 3e | Cl | Piperidine | 3.0 | 11.1 | 10.7 | 18.7 |
| 3f | Cl | Pyrrolidine | 15.2 | 4.6 | 4.3 | 9.6 |
| 3g | Cl | Morpholine | 22.7 | 0.8 | 4.3 | 3.4 |
| 3h | Cl | N,N-Diethylamine | 42.4 | 4.8 | 5.6 6.4 | |
| 3i | F | Piperidine | 40.9 | −4.7 | −6.0 5.1 | |
| 3j | F | Pyrrolidine | 33.3 | 5.0 | 4.3 | −2.7 |
| 3k | F | Morpholine | 56.1 | 3.8 | 0.7 | 3.2 |
| 3l | F | N,N-Diethylamine | 18.2 | 11.6 | 14.5 | 7.9 |
| 3m | CH3 | Piperidine | 31.8 | 6.8 | 10.5 | 2.4 |
| 3n | CH3 | Pyrrolidine | 65.2 | 1.9 | 4.7 | 6.1 |
| 3o | CH3 | Morpholine | 57.6 | 8.0 | 7.8 | 3.5 |
| 3p | CH3 | N,N-Diethylamine | 51.5 | 11.5 | 10.2 | 11.2 |
| 5a | H | – | 3.0 | 6.5 | 10.3 | 45.8 |
| 5b | Cl | – | 7.6 | 24.4 | 28.9 | 24.8 |
| 5c | F | – | 9.1 | −0.6 | −3.6 | 7.4 |
| 5d | CH3 | – | 71.2 | −1.0 | 6.7 | 7.1 |
| 7a | H | – | 98.5 | 9.0 | 10.1 | −3.2 |
| 7b | F | 100.0 | 2.1 | 5.0 | 3.0 | |
| 7c | Cl | – | 100.0 | 6.1 | 1.2 | 1.4 |
| 7d | CH3 | – | 59.1 | 1.3 | 8.1 | 8.2 |
| 7e | NO2 | – | 60.6 | 0.5 | 3.2 | 4.8 |
| GDC-0941 | 30.2 | 56.8 | 72.2 | |||