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Immune checkpoint inhibitory effects of the synthesized compounds on the gene expression of CTLA-4 and PD-L1.
| Compound | IC50 (μM) against CTLA-4 a | IC50 (μM) against PD-L1 b |
|---|---|---|
| 1 | 49 | 57 |
| 2a | >50 | >50 |
| 2b | 36 | 37 |
| 2c | >50 | >50 |
| 2d | >50 | >50 |
| 2e | 26 | 31 |
| 2f | 36 | 23 |
| 2g | >50 | >50 |
| 2h | >50 | 41 |
| 2i | >50 | 46 |
| 2j | >50 | >50 |
| 3a | 31 | 47 |
| 3b | 18 | 20 |
| 3c | 26 | 18 |
| 3d | 21 | 21 |
| 3e | 20 | 14 |
| 5 | 30 | 27 |
| 6 | >50 | 42 |
| 7 | 39 | 25 |
| 12 | 18 | 9.0 |
| 13 | 18 | 8.7 |
On HEK293 cells transfected with pCTLA-4–luciferase.
On A549 cells transfected with pPD-L1–luciferase.
