Table 3. Antiproliferation Activities for 2–6 against Drug-Resistant Tumor Cellsa.
| IC50 (nM) |
selectivity ratio |
|||||||
|---|---|---|---|---|---|---|---|---|
| compd | A2780/CDDP | MDA-MB-231/Gem | MCF-7/ADR | KB-V | IC50(A2780)/IC50(A2780/CDDP) | IC50(MDA-MB-231)/IC50(MDA-MB-231/Gem) | IC50(MCF-7)/IC50(MCF-7/ADR) | IC50(KB)/IC50(KB-V) |
| 15 | 4820 | 4747 | 7845 | 1959 | 0.3 | 0.3 | 0.5 | 1.9 |
| 1 | 85.7 | 85.9 | 156.8 | 24.9 | 0.2 | 1.0 | 2.8 | 5.1 |
| 2 | 94.0 | 25.2 | 16.3 | 16.0 | 0.1 | 0.2 | 144.2 | 283.9 |
| 3 | 22.8 | 6.9 | 5.1 | 11.0 | 0.3 | 0.1 | 559.4 | 294.0 |
| 4 | 47.2 | 50.4 | 50.1 | 65.4 | 0.2 | 0.02 | 62.5 | 17.5 |
| 5 | 51.7 | 10.5 | 18.0 | 13.9 | 0.2 | 0.05 | 103.6 | 157.0 |
| 6 | 34.1 | 93.0 | 47.9 | 10.1 | 0.4 | 0.02 | 29.5 | 164.9 |
| cisplatin | 201370 (r.r. = 79) | NA | NA | NA | NA | NA | NA | NA |
| doxorubicin | NA | NA | >100000 (r.r. > 113) | NA | NA | NA | NA | NA |
| gemcitabine | NA | >50000 (r.r. > 1373) | NA | NA | NA | NA | NA | NA |
| vincristine | NA | NA | NA | 417.0 (r.r. = 646) | NA | NA | NA | NA |
a
MTT assay. The data are the mean of triplicate determinations. r.r.: resistant ratio; r.r. = IC50 (drug-resistant cell lines)/IC50 (drug-sensitive cell lines). NA: not available. A2780/CDDP: cisplatin resistant human ovarian cancer cell lines. MDA-MB-231/Gem: gemcitabine resistant human breast cancer cell lines. MCF-7/ADR: doxorubicin resistant human breast cancer cell lines. KB-V: vincristine resistant human oral epidermoid cancer cell lines.