Table 7.
Cytotoxic activity of derivatives 14a–14h in human tumor cell lines (leukemia and breast) and in primate non-tumor kidney Vero cells a.
| |||||||
|---|---|---|---|---|---|---|---|
| Leukemia | Breast | Vero | |||||
| Compounds | HL60 | HEL | K-562 | BT549 | MCF7 | SKBR3 | |
| 4g (R3 = Ph) | 1.75 ± 0.21 | 1.00 ± 0.42 | 2.55 ± 0.78 | 3.55 ± 0.64 | >10 | >10 | >25 |
| 14a (R3 = 4-Cl-Ph) | 4.20 ± 0.85 | 4.20 ± 1.27 | 3.65 ± 0.21 | ND | 1.52 ± 0.54 | 5.70 ± 0.99 | 10.81 ± 1.26 |
| 14b (R3 = 4-Br-Ph) | 5.00 ± 0.14 | 5.45 ± 1.48 | 5.45 ± 0.78 | 9.55 ± 0.07 | 2.14 ± 0.08 | 7.25 ± 2.33 | >25 |
| 14c (R3 = 4-CF3-Ph) | 1.95 ± 0.07 | 2.75 ± 0.07 | 2.10 ± 0.57 | 4.60 ± 2.83 | 0.59 ± 0.00 | 2.30 ± 0.71 | 10.29 ± 2.21 |
| 14d (R3 = 3-F-Ph) | 1.05 ± 0.64 | 2.15 ± 0.92 | 0.95 ± 0.4 | >10 | 0.96 ± 0.19 | 2.01 ± 1.12 | 11.44 ± 1.25 |
|
14e (R3 = 4-OMe-Ph) |
1.10 ± 0.14 | 1.95 ± 0.07 | 2.95 ± 0.4 | 4.4 ± 1.34 | 0.85 ± 0.03 | 2.40 ± 0.28 | >25 |
|
14f (R3 = 4-(Me2N)-Ph |
4.00 ± 0.99 | 5.60 ± 2.12 | >10 | ND | 3.15 ± 2.15 | 8.00 ± 2.40 | 24.66 ± 0.49 |
| 14g (R3 = 2-furyl) | 1.10 ± 0.04 | 2.25 ± 0.78 | 2.30 ± 0.57 | 6.90 ± 2.50 | 0.93 ± 0.74 | 2.30 ± 0.42 | 13.69 ± 8.56 |
| 14h (R3 = CH3) | 3.90 ± 0.57 | 3.90 ± 0.28 | 4.4 ± 1.48 | >10 | 1.83 ± 0.62 | 5.25 ± 0.64 | 3.34 ± 0.54 |
a Expressed as IC50 values given in μM and determined as means ± SD (n = 3). ND: not determined.