Table 2. EGFR and HER-2 inhibitory activity and selectivity index with anti-proliferation activity of the synthesized compounds (C1-C20).
| Compounds | IC50(μM) | IC50(μM) | GI50(μM) | GI50(μM) | SI |
|---|---|---|---|---|---|
| EGFR | HER-2 | MDA-MB-453 | MCF-7 | EGFR/HER-2 | |
| C1 | 21.85 ± 2.03 | 16.01 ± 1.45 | 63.4 ± 6.12 | 10.03 ± 0.91 | 1.36 |
| C2 | 2.94 ± 0.26 | 0.56 ± 0.05 | 2.20 ± 0.18 | 4.68 ± 0.42 | 5.25 |
| C3 | 4.42 ± 0.35 | 7.18 ± 0.65 | 19.9 ± 1.84 | 5.30 ± 0.49 | 0.62 |
| C4 | 59.33 ± 5.58 | 125.3 ± 10.2 | >300 | 185.4 ± 17.8 | 0.47 |
| C5 | 43.58 ± 4.10 | 86.55 ± 8.05 | 135.1 ± 11.1 | 57.2 ± 5.36 | 0.50 |
| C6 | 4.49 ± 0.41 | 0.06 ± 0.004 | 0.20 ± 0.02 | 4.95 ± 0.43 | 74.8 |
| C7 | 9.45 ± 0.88 | 62.85 ± 5.67 | >300 | 16.8 ± 0.98 | 0.15 |
| C8 | 8.63 ± 0.78 | 0.45 ± 0.04 | 1.69 ± 0.15 | 5.64 ± 0.52 | 19.2 |
| C9 | 65.16 ± 5.88 | 0.37 ± 0.03 | 1.38 ± 0.12 | 56.2 ± 5.41 | 176.1 |
| C10 | 37.95 ± 3.75 | 0.08 ± 0.006 | 0.25 ± 0.02 | 18.2 ± 1.71 | 474.4 |
| C11 | 47.83 ± 4.54 | 1.90 ± 0.15 | 11.9 ± 1.05 | 28.5 ± 2.80 | 25.2 |
| C12 | 53.82 ± 5.12 | 0.84 ± 0.07 | 5.31 ± 0.48 | 33.9 ± 3.21 | 64.1 |
| C13 | 82.03 ± 7.84 | 0.80 ± 0.07 | 3.24 ± 0.30 | 123.3 ± 11.2 | 102.5 |
| C14 | 84.26 ± 7.81 | 1.23 ± 0.10 | 9.12 ± 0.89 | 134.7 ± 11.6 | 68.5 |
| C15 | 27.50 ± 2.46 | 0.29 ± 0.02 | 0.95 ± 0.08 | 12.1 ± 1.17 | 94.8 |
| C16 | 10.20 ± 0.94 | 0.13 ± 0.01 | 0.36 ± 0.03 | 5.99 ± 0.55 | 78.5 |
| C17 | 79.71 ± 7.01 | 0.21 ± 0.02 | 0.55 ± 0.02 | 96.4 ± 9.22 | 379.6 |
| C18 | 34.03 ± 3.08 | 0.96 ± 0.08 | 8.68 ± 0.84 | 15.2 ± 1.40 | 35.4 |
| C19 | 196.5 ± 18.5 | 12.04 ± 1.02 | 33.4 ± 2.95 | >300 | 16.3 |
| C20 | 28.56 ± 2.52 | 0.03 ± 0.002 | 0.15 ± 0.01 | 11.9 ± 1.06 | 952.0 |
| Erlotinib | 0.03 ± 0.003 | 0.16 ± 0.01 | 1.56 ± 0.14 | 0.08 ± 0.006 | 0.19 |
| Lapatinib | 0.01 ± 0.001 | 0.01 ± 0.001 | 0.03 ± 0.002 | 3.12 ± 0.24 | 1.00 |