Table 2.
In Vitro Inhibitory Effects of Modificated ATCAA Compounds against the Proliferation of Melanoma (A 375, B16-F1) and Prostate Cancer Cells (DU145, PC-3, LNCaP, PPC-1).
 |
A ring | B ringa | C ringb | X | IC50 ± SEM (μM) |
|||||
|---|---|---|---|---|---|---|---|---|---|---|
| B16-F1 | A375 | DU 145 | PC-3 | LNCaP | PPC-1 | |||||
| ATCAA-1 | p-NHAc-Ph | TZD | C16H33 | CONH | 2.2±0.3 | 2.1±0.2 | 1.7 ± 0.1 | 1.2 ± 0.1 | 1.0 ± 0.1 | 0.4 ± 0.1 |
| ATCAA-2 | p-NHAc-Ph | TZD | 9H-fluoren-1-yl | CONH | 3.9±0.3 | 2.1±0.1 | 1.9 ± 0.3 | 2.1 ± 0.1 | 3.5 ± 0.7 | 1.6 ± 0.1 |
| 2a | Ph | TZD | 3,4,5-trimethoxyl-Ph | CONH | >100 | >100 | >20 | >20 | >20 | >20 |
| 2b | 3,4,5-trimethoxyPh | TZD | 3,4,5-trimethoxyl-Ph | CONH | >100 | >100 | >20 | >20 | >20 | >20 |
| 4a(4R) | Ph | TZL | 3,4,5-trimethoxyl-Ph | CONH | 38.3± 3.2 | 22.8±1.6 | >20 | >20 | >20 | 5.3± 0.3 |
| 4b(4S) | Ph | TZL | 3,4,5-trimethoxyl-Ph | CONH | 30.4±2.8 | 13.6±1.2 | >20 | 13.2± 2.1 | 16.8± 1.8 | 3.4± 0.2 |
| 5 | Ph | TZ | 3,4,5-trimethoxyl-Ph | CONH | >100 | >100 | >20 | >20 | >20 | >20 |
| 8f | Ph | TZ | 3,4,5-trimethoxyl-Ph | CO | 0.055 ± 0.005 | 0.028 ± 0.005 | 0.071 ± 0.004 | 0.021 ±0.001 | 0.028 ± 0.004 | 0.043 ± 0.005 |
| Colchicine | 0.029 ± 0.005 | 0.020 ± 0.003 | 0.010 ± 0.002 | 0.011 ± 0.001 | 0.016 ± 0.004 | 0.020 ± 0.001 | ||||
a
TZD=Thiazolidine, TZL=Thiazoline, TZ= Thiazole
b
For ATCAA-1, “C” position contains a lipid chain.