Table 1.
Cytotoxicity activity (GI50a values, in μg·mL−1) and selective index (SIb; given in parentheses) of functionalized piperidines and doxorubicin (DOX)c against cancer cell lines.
| Compound | Cell lined |
|||||||
|---|---|---|---|---|---|---|---|---|
| U251 | MCF7 | NCI/ADR-RES | 786–0 | NCI-H460 | PC-3 | HT29 | HaCaT | |
| 1 | >250 | >250 | >250 | 113.9 (>2.2) | >250 | 6.3 (>39.7) | >250 | >250 |
| 2 | >250 | >250 | >250 | 20.0 (>12.5) | >250 | 17.2 (>14.5) | >250 | >250 |
| 3 | >250 | >250 | >250 | 23.0 (>10.9) | >250 | 7.8 (>32.0) | >250 | >250 |
| 4 | >250 | >250 | >250 | 160.7 (>1.5) | >250 | 56.9 (>4.4) | >250 | >250 |
| 5 | >250 | >250 | >250 | 71.8 (>3.5) | >250 | >250 | >250 | >250 |
| 6 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 |
| 7 | 181.8 (0.5) | 48.9 (2.0) | 38.7 (2.5) | 62.1 (1.5) | 94.7 (1.0) | 14.4 (6.7) | 111.0 (0.9) | 95.9 |
| 8 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 |
| 9 | >250 | >250 | >250 | 74.7 (>3.3) | >250 | >250 | >250 | >250 |
| 10 | >250 | 39.4 (>6.3) | >250 | 14.2 (>17.6) | >250 | 25.0 (>10.0) | 83.5 (>3.0) | >250 |
| 11 | >250 | >250 | 194.8 (>1.3) | 241.9 (>1.0) | >250 | >250 | >250 | >250 |
| 12 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 |
| 13 | >250 | 189.8 (>1.3) | 48.7 (>5.1) | >250 | >250 | 39.0 (>6.4) | 69.1 (>3.6) | >250 |
| 14 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 |
| 15 | >250 | >250 | 90.5 (>2.7) | 166.8 (>1.5) | >250 | >250 | >250 | >250 |
| 16 | 208.5 (0.3) | 26.2 (2.4) | 17.5 (3.6) | 0.4 (156.0) | 57.3 (1.9) | 10.2 (6.1) | 4.1 (15.2) | 62.4 |
| 17 | 193.8 (0.1) | >250 | >250 | 12.1 (10.8) | 207.2 (0.6) | >250 | >250 | 130.8 |
| 18 | >250 | >250 | >250 | 63.2 (>4.0) | >250 | >250 | >250 | >250 |
| 19 | >250 | 71.5 (>3.5) | >250 | 46.9 (>5.3) | >250 | 134.2 (>1.9) | 106.2 (>2.3) | >250 |
| 20 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 |
| 21 | 96.7 (0.4) | 45.5 (0.8) | 71.7 (0.5) | 82.5 (0.5) | 112.6 (0.3) | 16.0 (0.4) | 188.3 (0.2) | 38.6 |
| 22 | 58.2 (1.1) | 67.6 (0.9) | 19.8 (3.1) | 54.4 (1.1) | 26.3 (2.3) | 10.6 (5.8) | 90.0 (0.7) | 62.0 |
| 23 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 |
| 24 | >250 | 146.0 (>1.7) | >250 | >250 | >250 | 45.5 (>5.5) | >250 | >250 |
| 25 | >250 | >250 | 23.3 (>10.9) | >250 | >250 | 6.4 (>39.1) | >250 | >250 |
| DOXb | 0.03 (1.0) | 0.07 (0.4) | 0.3 (0.1) | 0.03 (1.0) | 0.01 (3.0) | 0.1 (0.3) | 0.2 (0.1) | 0.03 |
a
GI50 is the concentration of compound (μg·mL−1) that inhibits cancer cell growth by 50%.
b
Selectivity index was determined as the ratio of the GI50 value for HaCat to the GI50 value obtained for the cancer cell line.
c
DOX is the reference drug doxorubicin.
d
U251, glioma cells; MCF7, breast cancer cells; NCI/ADR-RES, multiple drug-resistant ovarian cancer cells; 786-0, renal cancer cells; NCI-H460, non-small lung cancer cells; PC-3, prostate cancer cells; HT29, colon cancer cells; HaCat, human keratinocyte cells.