Table 2. Structures and RTKs inhibitory activities of title compounds (QDAU1-10, IC50, nM).
Compound | R1 | R2 | VEGFR-2 | Tie-2 | EphB4 |
---|---|---|---|---|---|
QDAU1 | H | 3-CF3 | 194 | 70.5 | >500 |
QDAU2 | H | 3-Cl | 57.9 | 83.9 | >500 |
QDAU3 | H | 3-F | >500 | 90.7 | 5.64 |
QDAU4 | H | 2-F | 1.91 | 4.91 | 13.9 |
QDAU5 | 3-F | 4-F | 0.77 | 8.87 | 3.21 |
QDAU6 | H | 4-F | 6.28 | 101 | >500 |
QDAU7 | H | 4-OCF3 | >500 | 258 | >500 |
QDAU8 | H | -CH(CH3)2 | 41.5 | >500 | >500 |
QDAU9 | 4-Cl | 3-CF3 | 15.8 | 19.6 | 24.4 |
QDAU10 | H | 4-CF3 | 50.7 | 52.7 | >500 |
Sorafenib | 0.55 | 4.65 | 3.00 |