Table 2.
Antiproliferative activity of synthetic quinazoline derivatives bearing various phenoxy-methylene-1,2,3-triazole pendants assessed by the SRB reduction assay.
| Compound | AsPc-1 | EBC-1 | MKN-45 | Mia-Paca-2 | HT-29 | K562 |
|---|---|---|---|---|---|---|
| IC50 (µM) | ||||||
| 8a | > 100 | > 100 | > 100 | > 100 | > 100 | 57.4 ± 21.9 |
| 8b | > 100 | > 100 | > 100 | > 100 | > 100 | > 100 |
| 8c | 15.3 ± 2.3 | 19.0 ± 0.7 | 22.0 ± 4.8 | 25.6 ± 2.4 | 21.0 ± 4.7 | 31.5 ± 6.4 |
| 8d | > 100 | > 100 | 83.6 ± 6.0 | > 100 | 93.4 ± 2.2 | > 100 |
| 8e | > 100 | > 100 | > 100 | > 100 | > 100 | 61.5 ± 21.6 |
| 8f | > 100 | > 100 | 56.6 ± 6.5 | > 100 | > 100 | > 100 |
| 8g | > 100 | > 100 | 67.7 ± 4.6 | > 100 | > 100 | 96.6 ± 1.1 |
| 8h | 9.7 ± 1.9 | 6.1 ± 1.0 | 12.0 ± 3.9 | 11.5 ± 0.8 | 8.6 ± 1.3 | 34.4 ± 6.4 |
| 8i | > 100 | 89.4 ± 4.3 | > 100 | > 100 | > 100 | 86.2 ± 3.0 |
| Crizotinib | 2.45 ± 1.3 | 0.006 ± 0.001 | 0.05 ± 0.003 | 2.36 ± 1.2 | ND | ND |
| Cabozantinib | 1.4 ± 0.1 | 0.059 ± 0.014 | 1.04 ± 0.06 | 3.8 ± 0.6 | 3.7 ± 0.67 | 4.0 ± 1.0 |
The results are expressed as mean ± S.EM.