Table 1.
In vitro antitumour activity of 5-fluorouracil, afatinib, and the tested compounds.
| IC50 (μM)a |
||||
|---|---|---|---|---|
| Compd no. | HepG2b | MCF-7c | HeLad | PC-3e |
| 5-FU | 7.9 ± 0.17 | 5.4 ± 0.20 | 4.8 ± 0.21 | 8.3 ± 0.35 |
| Afatinib | 5.4 ± 0.25 | 7.1 ± 0.49 | 6.2 ± 0.67 | 7.7 ± 0.57 |
| 4a | 27.3 ± 1.96 | 40.9 ± 2.79 | 25.7 ± 1.97 | 21.8 ± 1.68 |
| 4b | 20.0 ± 1.11 | 36.4 ± 2.60 | 18.8 ± 1.57 | 17.1 ± 1.58 |
| 5a | >100 | >100 | 77.8 ± 4.41 | 94.1 ± 5.82 |
| 5b | 55.4 ± 3.95 | 49.4 ± 3.16 | 30.1 ± 2.24 | 71.1 ± 4.93 |
| 5c | 71.3 ± 4.53 | 64.7 ± 4.27 | 37.5 ± 2.81 | 26.9 ± 1.89 |
| 6a | 15.9 ± 1.02 | 18.1 ± 1.58 | 9.4 ± 0.98 | 10.5 ± 0.97 |
| 6b | 13.0 ± 0.87 | 13.7 ± 1.35 | 6.7 ± 0.67 | 9.1 ± 0.88 |
| 7 | 8.0 ± 0.38 | 7.5 ± 0.54 | 10.3 ± 1.13 | 13.3 ± 1.26 |
| 8a | 18.9 ± 1.35 | 29.3 ± 1.97 | 16.2 ± 1.36 | 12.7 ± 1.13 |
| 8b | 7.2 ± 0.24 | 5.6 ± 0.36 | 5.5 ± 0.45 | 7.8 ± 0.56 |
| 9 | 62.3 ± 4.10 | 58.4 ± 4.50 | 46.2 ± 3.30 | 50.1 ± 3.55 |
| 10 | 80.9 ± 5.34 | 70.9 ± 4.98 | 51.2 ± 3.82 | 41.9 ± 2.87 |
| 11 | 92.9 ± 5.82 | 97.3 ± 5.51 | 62.4 ± 3.80 | 87.7 ± 5.41 |
| 12a | 85.4 ± 5.31 | 87.1 ± 5.24 | 89.4 ± 4.89 | >100 |
| 12b | 30.8 ± 2.07 | 48.1 ± 3.25 | 66.8 ± 4.07 | 69.4 ± 4.32 |
a
IC50, compound concentration required to inhibit tumour cell proliferation by 50% (mean ± SD, n = 3).
b
Human hepato-cellular carcinoma cell line (HepG2).
c
Human breast adenocarcinoma cell line (MCF-7).
d
Human cervical epithelioid carcinoma cell line (HeLa).
e
Human prostate cancer cell line (PC-3).
IC50, (μM): 1–10 (very strong), 11–25 (strong), 26–50 (moderate), 51–100 (weak), above 100 (non-cytotoxic).