Table 2.
Antitumor activity (GI50 / µM)a data of compounds 5f and 7; selected for 5 dose studies for the NCI 60-cell line screen
| 5f | 7 | |||
|---|---|---|---|---|
| Panel/cell line | GI50 | LC50b | GI50 | LC50 |
| Leukemia | ||||
| CCRF-CEM | 19.1 | >100 | 6.13 | 79.6 |
| HL-60(TB) | 21.7 | 99.9 | 6.90 | 77.5 |
| K-562 | 25.2 | >100 | 7.36 | 90.0 |
| MOLT-4 | 25.7 | >100 | 19.6 | 97.9 |
| RPMI-8226 | 19.7 | >100 | 17.0 | >100 |
| SR | 20.7 | >100 | 13.6 | >100 |
| Lung Cancer | ||||
| A549/ATCC | 29.8 | >100 | 19.8 | >100 |
| HOP-62 | 35.8 | >100 | 47.4 | >100 |
| NCI-H226 | 30.2 | >100 | 15.4 | 62.3 |
| NCI-H23 | 23.0 | >100 | 23.7 | >100 |
| NCI-H322M | 44.7 | >100 | 61.3 | >100 |
| NCI-H460 | 29.3 | >100 | 30.1 | >100 |
| NCI-H522 | 5.44 | 59.7 | 1.71 | 6.34 |
| Colon Cancer | ||||
| COLO 205 | 22.6 | 90.9 | 14.5 | 58.8 |
| HCC-2998 | 33.8 | >100 | NA | NA |
| HCT-116 | 28.3 | >100 | 11.8 | 49.0 |
| HCT-15 | 22.6 | >100 | 10.7 | 55.6 |
| HT29 | 27.0 | >100 | 17.6 | 61.5 |
| KM12 | 20.4 | 86.7 | 43.2 | >100 |
| SW-620 | 22.9 | >100 | 11.4 | 62.8 |
| CNS Cancer | ||||
| SF-268 | 21.3 | >100 | 23.0 | >100 |
| SF-295 | 28.5 | >100 | 32.1 | >100 |
| SF-539 | 16.1 | 62.2 | 16.7 | 60.8 |
| SNB-19 | 47.6 | >100 | >100 | >100 |
| SNB-75 | 21.5 | >100 | 19.3 | >100 |
| U251 | 21.7 | >100 | 36.7 | >100 |
| Melanoma | ||||
| LOX IMVI | 18.0 | 71.2 | 14.9 | 60.9 |
| MALME-3M | 22.5 | >100 | 10.9 | 62.7 |
| M14 | 20.5 | >100 | 16.5 | 65.6 |
| MDA-MB-435 | 18.3 | >100 | 13.8 | 59.5 |
| SK-MEL-2 | NA | NA | 18.6 | 66.1 |
| SK-MEL-28 | 29.4 | >100 | 16.1 | 73.0 |
| SK-MEL-5 | 16.3 | 60.4 | 18.5 | 95.6 |
| UACC-257 | 16.6 | >100 | 12.0 | 53.9 |
| UACC-62 | 13.8 | 76.6 | NA | NA |
| Ovarian Cancer | ||||
| IGROV1 | 27.9 | >100 | 20.0 | 75.6 |
| OVCAR-3 | 20.5 | >100 | 6.85 | 50.8 |
| OVCAR-4 | 24.3 | >100 | 13.2 | 60.0 |
| OVCAR-5 | 48.1 | >100 | 13.7 | 52.5 |
| OVCAR-8 | 26.9 | >100 | 16.6 | 59.9 |
| NCI/ADR-RES | 23.6 | >100 | 31.2 | >100 |
| SK-OV-3 | 44.9 | >100 | 47.3 | >100 |
| Renal Cancer | ||||
| 786-0 | 35.7 | >100 | 14.3 | 53.0 |
| A498 | 17.5 | >100 | 45.2 | >100 |
| ACHN | 32.8 | >100 | 10.5 | 47.4 |
| CAKI-1 | 30.9 | >100 | 6.61 | 49.5 |
| RXF 393 | 18.1 | >100 | NA | NA |
| SN12C | 25.8 | >100 | 17.7 | 84.1 |
| TK-10 | 34.7 | >100 | NA | NA |
| UO-31 | 27.3 | >100 | 10.8 | 50.0 |
| Prostate Cancer | ||||
| PC-3 | 22.7 | >100 | 23.1 | >100 |
| DU-145 | 25.7 | >100 | 18.8 | 68.3 |
| Breast Cancer | ||||
| MCF7 | 20.0 | >100 | 9.79 | >100 |
| MDA-MB-231/ATCC | 16.0 | 81.8 | 16.4 | 59.6 |
| HS 578T | 21.5 | >100 | 21.3 | >100 |
| BT-549 | 20.1 | 88.2 | 15.9 | 55.3 |
| T-47D | 29.5 | >100 | 9.88 | 54.3 |
| MDA-MB-468 | 17.7 | >100 | 11.1 | 60.4 |
na: Not analyzed;
a
GI50: 50% Growth inhibition, concentration of drug (µM) resulting in a 50% reduction in net cell growth as compared to cell numbers on day 0.
b
LC50 the drug concentration (µM) that was required to kill 50% of the cells.