Table 2.
Whole-cell HDAC inhibition (HDAC) and cytotoxic activity (MTT) against the human tongue squamous cell carcinoma cell line Cal27 of 4a–m, vorinostat, Nexturastat A and Tubastatin A.
| entry | R1 | R2 | HDAC (Cal27) IC50 [μM] | MTT (Cal27) IC50 [μM] |
|---|---|---|---|---|
| 4a |
|
H | 14.0(±1.40) | 3.64(±1.24) |
| 4b |
|
H | 14.8(±3.14) | 4.78(±1.70) |
| 4c |
|
H | 13.9(±2.93) | 4.53(±1.93) |
| 4d |
|
H | 14.0(±1.41) | 11.9(±2.72) |
| 4e |
|
H | 1.75(±0.27) | 3.22(±0.87) |
| 4f |
|
H | 14.8(±3.13) | 4.60(±1.60) |
| 4g |
|
H | >100 | 27.7(±8.23) |
| 4h |
|
H | >100 | >100 |
| 4i | H | H | 13.9(±2.93) | 4.61(±1.45) |
| 4j | H | 7-Me | 8.13(±1.08) | 3.92(±1.20) |
| 4k | H | 6-Me | 17.5(±1.85) | 4.21(±1.95) |
| 4l |
|
H | 27.6(±4.68) | 3.87(±1.15) |
| 4m |
|
H | 9.38(±3.03) | 3.83(±1.40) |
|
| ||||
| vorinostat | 0.87(±0.10) | 2.64 (±0.10)a | ||
| Nexturastat A | 5.87(±1.70) | 7.75(±1.56) | ||
| Tubastatin A | 11.4(±2.16) | 5.34(±0.74) | ||