Table 2.
Antiproliferative activities of cis-stilbene analogues.
| ||||||||
|---|---|---|---|---|---|---|---|---|
| DMU Code | R (A-Ring) | R’ (B-Ring) | IC50 (µM) a | AF | IC50 (µM) a | TS | ||
| MCF7 | MCF7 (TCDD) | MCF10A | MDA468 | |||||
| 265 | 4-OMe- | 4-OMe | 25 | 20 | 1 | >100 | >100 | 1 |
| 241C | 4-OMe- | 3-OMe | 29 | 26 | 1 | >100 | >100 | 1 |
| 216C | 4-OMe- | 3-Me | 26 | 30 | 1 | >100 | >100 | 1 |
| 210 | 4-OMe- | 3,5-(OMe)2 | 26 | 24 | 1 | >100 | >100 | 1 |
| 508 | C6H5 | 3,4,5-(OMe)2 | 5 | 4 | 1 | 7 | 9 | 0.9 |
| 213 | 4-OMe | 3,4,5-(OMe)3 | 2.5 | 0.44 | 6 | 2 | 0.5 | 4 |
| 548 | 4-OMe | 3,4,5-(OMe)3 | 8 | 7.1 | 1 | 100 | 30 | 3 |
| 261 | 4-OEt | 3,4,5-(OMe)3 | 0.04 | 0.13 | 0.3 | 0.06 | 0.07 | 0.9 |
| 556 | 4-Cl | 3,4,5-(OME)3 | 0.8 | 0.8 | 1 | 35 | 7 | 5 |
| 558 | 4-Br | 3,4,5-(OMe)3 | 0.08 | 0.05 | 2 | 0.05 | 0.04 | 1 |
| 510 | 4-I | 3,4,5-(OMe)3 | 0.06 | 0.06 | 1 | 0.01 | 0.006 | 2 |
| 568 | 6-OMe-Naphthyl- | 3,4,5-(OMe)3 | 0.05 | 0.05 | 1 | 100 | 1 | 100 |
| 570 | 4-OMe-Naphthyl- | 3,4,5-(OMe)3 | 0.82 | 0.45 | 1.8 | 100 | 4 | 25 |
| 1024 | 3,4-(OMe)2-Ph- | 3,4,5-(OMe)3 | 9 | 9 | 1 | 10 | 6 | 2 |
| 222 | 2,4-(OMe)2-Ph- | 3,4,5-OMe)3 | 0.07 | 0.007 | 10 | 0.06 | 0.005 | 10 |
| 299 | 3,4-OCH2O | 3,4,5-(OMe)3 | 0.05 | 0.05 | 1 | 20 | 20 | 1 |
| CA4 | 4-OMe-3-OH | 3,4,5-(OMe)3 | 0.002 | 0.002 | 1 | 0.002 | 0.003 | 0.7 |
a IC50 values are means of quadruplicate determinations, as measured by the MTT assay after 96 h incubation of the drug with the cells cultured at 37 °C; AF = activation factor = IC50 MCF7/MCF7 (TCDD); TS = tumour selectivity = IC50 MCF10A/IC50 MDA468.