The antiproliferative activity of benzylamine-modified tirbanibulin analogs against HeLa cells.
| |||||||
|---|---|---|---|---|---|---|---|
| Compound | R | HeLa IC50a,b (μM) | cLogPc | Compound | R | HeLa IC50a,b (μM) | cLogPc |
| 8 |
|
0.044 ± 0.011 | 3.3 | 48 |
|
0.27 ± 0.07 | 4.0 |
| 39 |
|
>4.0 | 2.8 | 49 |
|
2.0 ± 0.5 | 3.2 |
| 40 |
|
>4.0 | 2.8 | 50 |
|
0.15 ± 0.04 | 2.7 |
| 41 |
|
2.1 ± 0.6 | 3.0 | 51 |
|
0.63 ± 0.07 | 2.0 |
| 42 |
|
2.2 ± 0.5 | 3.5 | 52 |
|
0.48 ± 0.06 | 3.4 |
| 43 |
|
0.97 ± 0.22 | 3.5 | 53 |
|
>4.0 | 4.2 |
| 44 |
|
0.027 ± 0.004 | 3.5 | 54 |
|
0.45 ± 0.10 | 3.6 |
| 45 |
|
0.26 ± 0.06 | 3.4 | 55 |
|
>4.0 | 3.6 |
| 46 |
|
0.53 ± 0.15 | 3.4 | 56 |
|
0.25 ± 0.06 | 3.6 |
| 47 |
|
0.040 ± 0.009 | 3.4 | 57 |
|
0.34 ± 0.11 | 3.3 |
a
Data represent the mean of three independent determinations from triplicate samples.
b
IC50 values were determined using the CCK-8 assay in HeLa cells.
c
cLogP values were calculated using online ALOGPS 2.1 program.