The activities of the novel compounds over normal cells (WI-38) and 3 cancer cell lines and the values of their IC50 (μM) are provided.
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|---|---|---|---|---|---|
| Comp. | R | IC50a (μM) | |||
| HCT-116 | HeLa | MCF-7 | WI-38 | ||
| 7a | CH3, X = N | 65.80 ± 3.8 | 52.40 ± 3.4 | 55.96 ± 3.2 | >100 |
| 7b | n-Propyl, X = N | 62.61 ± 3.6 | 45.71 ± 2.4 | 53.85 ± 2.8 | 32.79 ± 2.1 |
| 7c | Phenyl, X = N | 7.03 ± 0.6 | 9.88 ± 0.6 | 6.93 ± 0.4 | 43.93 ± 2.4 |
| 7d | None, X = CH2 | 73.89 ± 4.2 | 59.10 ± 3.3 | 67.34 ± 3.4 | 36.45 ± 2.0 |
| 7e | None, X = O | 88.43 ± 4.5 | 78.54 ± 4.2 | 84.68 ± 4.1 | 26.32 ± 1.9 |
| 9a | H | 44.35 ± 2.6 | 25.19 ± 2.0 | 37.21 ± 2.3 | 48.35 ± 2.6 |
| 9b | Cl | >100 | 87.68 ± 4.4 | >100 | 64.72 ± 3.5 |
| 9c | CH3 | 58.50 ± 3.3 | 51.93 ± 2.8 | 46.05 ± 2.5 | 18.11 ± 1.3 |
| 9d | OCH3 | >100 | 82.39 ± 4.1 | 92.38 ± 4.4 | >100 |
| 11a | 4-Br | 41.03 ± 2.4 | 33.41 ± 2.3 | 30.49 ± 2.1 | 75.94 ± 4.1 |
| 11b | 4-Cl | 12.61 ± 1.0 | 17.52 ± 1.4 | 8.39 ± 0.6 | 56.23 ± 3.0 |
| 11c | 4-CH3 | 21.51 ± 1.5 | 19.24 ± 1.6 | 9.15 ± 0.7 | 45.03 ± 2.4 |
| 11d | 4-OCH3 | 47.87 ± 2.7 | 63.42 ± 3.6 | 34.63 ± 2.3 | 71.23 ± 3.9 |
| 11e | 3,4-diOCH3 | 8.89 ± 0.8 | 13.64 ± 1.1 | 5.92 ± 0.3 | 60.30 ± 3.3 |
| 11f | 3-Br | 31.16 ± 2.2 | 35.88 ± 2.2 | 22.16 ± 1.6 | 77.28 ± 4.3 |
| 13a | H | 15.03 ± 1.2 | 23.59 ± 1.9 | 18.63 ± 1.3 | 91.39 ± 4.9 |
| 13b | CH3 | 29.32 ± 2.0 | 39.01 ± 2.4 | 27.82 ± 2.0 | 83.54 ± 4.5 |
| 13c | NO2 | 6.10 ± 0.5 | 10.33 ± 0.9 | 2.42 ± 0.1 | 38.65 ± 2.2 |
| 13d | Cl | 24.79 ± 1.8 | 42.92 ± 2.5 | 14.21 ± 1.1 | 66.08 ± 3.8 |
| 13e | Br | 55.07 ± 3.5 | 57.41 ± 3.2 | 42.56 ± 2.4 | >100 |
| DOX | 5.23 ± 0.3 | 5.57 ± 0.4 | 4.17 ± 0.2 | 6.72 ± 0.5 | |
a
The concentration required to prevent 50% of cancer cells from proliferating is known as the IC50 value. The mean ± SD from the dose–response curves of three separate trials is used to illustrate the data. IC50, expressed in μg mL−1, ranges from 1–10 (extremely strong), 11–20 (strong), 21–50 (moderate), and 51–100 (weak).