Table 5.
Cytotoxicity of optimized compounds on HUVECs (induced by 20 ng/mL VEGFA-165), HBVPs (induced by 20 ng/mL PDGF-BB) and inhibition of optimized compounds on VEGFR2/FGFR1/PDGFRβ.
| Compd. | IC50 |
||||
|---|---|---|---|---|---|
| VEGFR2 (nmol/L) | FGFR1 (nmol/L) | PDGFRβ (nmol/L) | HUVECs (nmol/L) | HBVPs (μmol/L) | |
| Lead compd. | 9.4 | 188.0 | 143.0 | 90.2 | / |
| D4/WXFL-152 | 7.0 | 69.0 | 31.0 | 71.0 | 1.94 |
| A1 | 20.1 | 293.7 | 67.6 | 228.8 | / |
| B2 | 26.7 | 216.4 | 56.9 | 145.9 | / |
| C2 | 78.6 | 63 | 311.1 | >10,000.0 | / |
| C3 | 10.0 | 129.9 | 84.3 | 31.0 | / |
| C4 | 22.6 | 378.4 | 139.9 | 30.9 | / |
| C16 | 20.5 | 1103.50 | 161.4 | 20.7 | / |
| C25 | 74.1 | 6100.40 | 193.7 | 84.1 | / |
| Nintedanib | 8.8 | 93.9 | 35.4 | 41.0 | 1.67 |