Table 2.
Structures, synthetic yields (methods A or B) and antiproliferative activities of second generation compounds 3
| # logP | structure | % yield (method) | cell viabilitya GI50, μM
|
# logP | structure | % yield (method) | cell viabilitya GI50, μM
|
||
|---|---|---|---|---|---|---|---|---|---|
| HeLa | MCF7 | HeLa | MCF7 | ||||||
| 3aafe |
|
73 (A) | 0.68 | 1.4 | 3aaff |
|
60 (A) | 26.9 | 2.4 |
| 6.7 | 61 (B) | ±0.04 | ± 0.1 | 4.9 | 56 (B) | ± 0.3 | ± 0.1 | ||
| 3aafg |
|
76 (A) | 18.2 | 6.3 | 3aafh |
|
84 (A) | 31.0 | 4.9 |
| 5.4 | 64 (B) | ± 0.9 | ± 1.1 | 5.9 | 72 (B) | ± 0.2 | ± 0.1 | ||
| 3aafi |
|
45 (A) | 31.7 | 12.2 | 3aafc |
|
75 (A) | 32.9 | 20.4 |
| 6.5 | 43 (B) | ± 1.7 | ± 1.0 | 4.1 | 64 (B) | ± 1.1 | ± 0.1 | ||
| 3aafj |
|
56 (A) | 27.4 | 10.2 | 3aafk |
|
70 (A) | 2.7 | 2.5 |
| 6.3 | 52 (B) | ± 0.2 | ± 0.1 | 6.1 | 59 (B) | ± 0.1 | ± 0.1 | ||
| 3aafd |
|
57 (A) | 13.0 | 2.7 | 3aafl |
|
81 (A) | 17.3 | 8.5 |
| 6.2 | 55 (B) | ± 0.4 | ± 0.0 | 5.6 | 72 (B) | ± 0.2 | ± 0.3 | ||
| 3aafm |
|
80 (A) | 6.3 | 4.9 | 3aafn |
|
76 (A) | 6.9 | 7.4 |
| 5.7 | 72 (B) | ± 1.3 | ± 0.2 | 5.7 | 69 (B) | ± 0.4 | ± 0.6 | ||
| 3aafo |
|
53 (A) | 4.1 | 7.9 | 3aafp |
|
45 (A) | 0.60 | 1.1 |
| 6.0 | 50 (B) | ± 0.2 | ± 0.7 | 5.3 | 43 (B) | ±0.02 | ± 0.0 | ||
| 3cafa |
|
83 (A) | 5.6 | 7.8 | 3dafa |
|
80 (A) | 9.8 | 9.3 |
| 6.8 | ± 0.3 | ± 0.6 | 6.7 | ± 0.8 | ± 0.3 | ||||
| 3cafe |
|
68 (A) | 6.6 | 7.7 | 3eafa |
|
75 (A) | 5.4 | 5.5 |
| 8.4 | ± 0.5 | ± 0.4 | 7.0 | ± 0.3 | ± 0.2 | ||||
a
Concentration required to reduce the viability of cells by 50% after a 48 h treatment with the indicated compounds relative to a DMSO control ± SD from two independent experiments, each performed in 4 replicates, as determined by the MTT assay.