Table 1.
Structures, synthetic yields (methods A or B) and antiproliferative activities of the first generation compounds 3
| # logP | structure | % yield (method) | cell viability GI50,a μM
|
# logP | structure | % yield (method) | cell viability GI50,a μM
|
||
|---|---|---|---|---|---|---|---|---|---|
| HeLa | MCF7 | HeLa | MCF7 | ||||||
| 3aaaa |
|
82 (A) | 23.0 | 31.0 | 3aaab |
|
73 (A) | >50 | >50 |
| 4.1 | 76 (B) | ± 2.6 | ± 0.6 | 4.1 | 68 (B) | ||||
| 3aaba |
|
68 (A) | >50 | >50 | 3aaca |
|
43 (A) | >50 | >50 |
| 4.1 | 61 (B) | 4.1 | 35 (B) | ||||||
| 3aada |
|
46 (A) | >50 | >50 | 3aaea |
|
76 (A) | 25.7 | 32.0 |
| 2.7 | 27 (B) | 5.2 | 70 (B) | ± 1.6 | ± 0.9 | ||||
| 3aafa |
|
85 (A) | 3.6 | 3.4 | 3abfa |
|
79 (A) | >50 | >50 |
| 4.1 | 73 (B) | ± 0.5 | ± 0.3 | 5.7 | 73 (B) | ||||
| 3acfa |
|
28 (B) | >50 | >50 | 3bafc |
|
54 (A) | 36.8 | 25.7 |
| 5.2 | 5.5 | ± 0.4 | ± 1.4 | ||||||
| 3bafa |
|
75 (A) | 19.7 | 10.0 | 3bafd |
|
36 (A) | 24.0 | 11.2 |
| 5.4 | ± 1.7 | ± 0.3 | 6.2 | ± 0.2 | ± 0.9 | ||||
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.