Table 3 Selected small molecules with excellent kinase inhibition activity
From: Angiogenic signaling pathways and anti-angiogenic therapy for cancer
Compounds | Chemical Structures | Targets | IC50 | References |
|---|---|---|---|---|
1 |
| VEGFR-2 | 0.19 nM | |
2 |
| VEGFR-2 | 2.6 nM | |
3 |
| VEGFR-2 | 3.2 nM | |
4 |
| VEGFR-2 | 3.2 nM | |
5 |
| VEGFR-2 | 27 nM | |
6 |
| VEGFR-2 | 66 nM | |
7 |
| VEGFR-2 | 0.12 μM | |
8 |
| VEGFR-2 | 0.12 μM | |
9 |
| VEGFR-2 | 0.23 μM | |
10 |
| VEGFR-2 | 0.29 μM | |
11 |
| VEGFR-2 | 0.31 μM | |
12 |
| VEGFR-2 PDGFR-β | 24.7 nM 16.1 nM | |
13 |
| VEGFR-2 FGFR-1 PDGFR-β | 7 nM 69 nM 31 nM | |
14 |
| VEGFR-2 FGFR-1 PDGFR-β | 0.18 μM 0.23 μM 0.1 μM | |
15 |
| VEGFR-2 c-Met PDGFR-β | 435 nM 654 nM 371 nM | |
16 |
| VEGFR-2 Tie-2 EphB4 | 1.05 nM 2.47 nM 0.27 nM | |
17 |
| VEGFR-2 Tie-2 EphB4 | 1.85 nM 0.73 nM 2.99 nM | |
18 |
| VEGFR-2 Tie-2 EphB4 | 2.35 nM 5.63 nM 3.87 nM | |
19 |
| VEGFR-2 HDAC4 | 5 μM 0.36 μM | |
20 |
| FGFR-4 | 5.4 nM | |
21 |
| FGFR-1 FGFR-2 VEGFR-2 | 1.0 nM 4.5 nM 2.9 nM | |
22 |
| FGFR-1 FGFR-2 FGFR-3 | 0.6 μM 1.3 μM 4.1 μM | |
23 |
| HIF-1α | 0.6 μM | |
24 |
| HIF-1α | 0.32 μM | |
25 |
| HIF-1α | 0.6 μM |
