Table 1. Affinity (Ki) for PCP Binding Site of NMDA Receptora and Cytotoxic Activity against MCF-7 and SKBR3 Breast Cancer Cell Linesb of 1–3 and Reference Compounds (S)-(+)-Ketamine and MK-801.
| PCP site of the NMDA receptora | MCF-7
(SKBR3) |
|||
|---|---|---|---|---|
| compd | Ki, nM | GI50, μM | TGI, μM | LC50, μM |
| 1 | 712 ± 99a | 74.4 ± 3.4 | 137.3 ± 5.6 | 253.1 ± 5.1 |
| (31.2 ± 5.3) | (200 ± 7.1) | (>300) | ||
| 2 (trans) | 413 ± 20a | 65.3 ± 2.3 | 107.2 ± 5.1 | 176.0 ± 6.1 |
| (23.8 ± 1.9) | (191.8 ± 4.3) | (>300) | ||
| 3 (cis) | 893 ± 40a | 89.7 ± 1.9 | 148 ± 4.7 | 244.2 ± 5.3 |
| (25.8 ± 2.1) | (180.3 ± 8.9) | (>300) | ||
| (S)-(+)-ketamine | 419 ± 4a | >300 | >300 | >300 |
| (>300) | (>300) | (>300) | ||
| MK-801 | 1.5 ± 0.1 | >300 | >300 | >300 |
| (>300) | (>300) | (>300) | ||
a
From ref (19).
b
In vitro cytotoxic activity in human MCF-7 and SKBR3 cells was carried out using SRB assay. Growth Inhibition 50 (GI50) represents the drug concentration (μM) required to inhibit 50% net of cell growth. Total growth inhibition (TGI) represents the drug concentration (μM) required to inhibit 100% of cell growth. Lethal concentration 50 (LC50) represents the drug concentration (μM) required to kill 50% of the initial cell number. Each quoted value represents the mean of quadruplicate determinations ± standard error (SE) (n = 5).