Table 18.
Antiproliferative activity of prodrugs 33a, 33 and 34 on LNCaP (prostate cancer), DU145 (prostate cancer), MDA-MB-231 (triple negative breast adenocarcinoma), MCF-7 (breast cancer), and HCT-116 (colon cancer) cell lines. MCR-5 pd30 (fetal lung normal cell line) was used as a reference. Selectivity index (SI) = IC50 MCR-5 pd30/average IC50 (LNCaP and DU145).
| Compound/ Cell Line |
IC50, µM | ||||||
|---|---|---|---|---|---|---|---|
| LNCaP | DU145 | MDA-MB-231 | MCF-7 | HCT116 | MCR-5 pd30 | SI | |
| 33 | 0.09 ± 0.02 | 0.15 ± 0.03 | 0.18 ± 0.01 | 0.45 ± 0.06 | 0.32 ± 0.08 | 2.2 ± 0.3 | 18.3 |
| 33a | 0.24 ± 0.06 | 0.19 ± 0.04 | 0.54 ± 0.06 | 0.7 ± 0.1 | 0.9 ± 0.1 | 3.8 ± 0.6 | 17.7 |
| 34 | 0.26 ± 0.03 | 0.27 ± 0.01 | 0.6 ± 0.1 | 0.8 ± 0.1 | 1.0 ± 0.2 | 3.6 ± 0.2 | 13.6 |
| Estramustine | 6 ± 1 | 11 ± 1 | 5.5 ± 0.9 | 12.6 ± 0.9 | 26 ± 2 | 25 ± 3 | 2.9 |
| Cisplatin | 2.4 ± 0.2 | 21 ± 3 | 14.8 ± 0.9 | 9 ± 1 | 2.4 ± 0.2 | 9 ± 2 | 2.6 |