Table 1.
In vitro antiproliferative activities (IC50, µM)a,b of the synthesised compounds 2–12.
Compound |
In vitro cytotoxicity (µM) |
WI38c | ||||
---|---|---|---|---|---|---|
HePG2 | HCT-116 | MCF-7 | PC3 | HeLa | ||
2 | 16.08 ± 1.4 | 8.81 ± 0.7 | 8.36 ± 0.9 | 26.82 ± 2.2 | 39.03 ± 2.4 | 86.48 ± 4.7 |
3 | 40.02 ± 2.5 | 10.84 ± 1.0 | 27.36 ± 1.8 | 44.50 ± 3.5 | 68.98 ± 3.9 | 63.1 ± 3.43 |
4 | 58.75 ± 3.3 | 72.40 ± 3.8 | 55.04 ± 3.2 | 14.27 ± 1.3 | 21.10 ± 1.6 | nt |
5 | 83.56 ± 4.4 | 94.14 ± 5.1 | >100 | 94.60 ± 4.9 | 75.19 ± 4.8 | nt |
6 | 79.04 ± 4.2 | 56.36 ± 3.2 | 81.58 ± 4.0 | >100 | 91.90 ± 5.1 | 204 ± 11.1 |
7 | 53.43 ± 2.9 | 38.63 ± 2.0 | 40.83 ± 2.5 | 70.10 ± 3.8 | 73.29 ± 4.2 | 59.49 ± 3.23 |
8 | 23.67 ± 1.8 | 13.85 ± 1.3 | 17.28 ± 1.4 | 36.69 ± 2.8 | 58.76 ± 3.7 | 151.4 ± 8.22 |
9 | 44.70 ± 2.7 | 29.52 ± 1.8 | 35.17 ± 2.2 | 51.06 ± 3.6 | 73.59 ± 4.1 | nt |
10 | 34.32 ± 2.1 | 27.49 ± 1.5 | 19.69 ± 1.6 | 30.90 ± 2.6 | 46.17 ± 3.0 | nt |
11 | 20.43 ± 1.6 | 46.13 ± 2.7 | 14.55 ± 1.3 | 18.75 ± 1.5 | 32.15 ± 1.9 | 94.49 ± 5.13 |
12 | 70.46 ± 3.8 | 49.72 ± 2.9 | 61.53 ± 3.5 | 93.48 ± 4.4 | 85.44 ± 4.7 | 76.26 ± 4.14 |
DOX | 4.50 ± 0.2 | 5.23 ± 0.3 | 4.17 ± 0.2 | 8.87 ± 0.6 | 5.57 ± 0.4 | 55.29 ± 3.0 |
Afatinib | 5.5 ± 0.24 | 11.2 ± 1.11 | 7.2 ± 0.50 | 7.6 ± 0.60 | 6.3 ± 0.69 | nt |
aIC50 values for each cell line are the compound concentration that inhibits 50% of the cell growth measured by MTT assay. bEach value was reproduced in triplicate. cNon tumour normal cell.