Table 2.
Antitumor activity (GI50/μM)a and toxicity (LC50/μM)b data of compounds selected for 5 dose studies for the NCI 57-cell lines screen
| Panel/cell line | Compound 3o | Compound 3n | ||
|---|---|---|---|---|
|
| ||||
| GI50 | LC50 | GI50 | LC50 | |
| Leukemia Cancer | ||||
| CCRF-CEM | 2.06 | >100 | 2.18 | >100 |
| HL-60(TB) | 3.22 | >100 | 4.91 | >100 |
| K-562 | 5.04 | >100 | 3.73 | >100 |
| MOLT-4 | 2.94 | >100 | 4.79 | >100 |
| RPMI-8226 | 2.62 | >100 | 2.87 | >100 |
| Non-Small Cell Lung Cancer | ||||
| A549/ATCC | 0.19 | 10.9 | 43.6 | >100 |
| EKVX | 28.5 | >100 | 71.7 | >100 |
| HOP-62 | 5.12 | >100 | 4.31 | >100 |
| NCI-H226 | 26.8 | >100 | 38.4 | >100 |
| NCI-H23 | 4.74 | >100 | 13.9 | >100 |
| NCI-H322M | 14.3 | >100 | 41.1 | >100 |
| NCI-H460 | 26.8 | >100 | 29.0 | >100 |
| NCI-H522 | 1.86 | 20.5 | 3.65 | >100 |
| Colon Cancer | ||||
| COLO 205 | 14.3 | >100 | 19.9 | >100 |
| HCC-2998 | 18.7 | 73.9 | 12.8 | 63.9 |
| HCT-116 | 3.00 | 34.5 | 2.40 | >100 |
| HCT-15 | 12.6 | >100 | 11.8 | >100 |
| HT29 | 1.38 | 44.1 | 4.06 | >100 |
| KM12 | 2.05 | 30.0 | 2.87 | 80.4 |
| SW-620 | 2.59 | 49.6 | 4.12 | >100 |
| CNS Cancer | ||||
| SF-268 | 3.31 | 64.9 | 5.00 | >100 |
| SF-295 | 3.71 | >100 | 26..0 | >100 |
| SF-539 | 3.12 | 79.1 | 3.73 | >100 |
| SNB-19 | 17.2 | >100 | 30.6 | >100 |
| SNB-75 | 3.39 | >100 | 28.8 | >100 |
| Melanoma Cancer | ||||
| LOX IMVI | 0.75 | 60.0 | 8.09 | >100 |
| MALME-3M | 29.6 | >100 | 27.4 | >100 |
| M14 | 3.59 | 61.4 | 4.93 | >100 |
| MDA-MB-435 | 6.12 | 93.1 | 10.6 | >100 |
| SK-MEL-2 | 10.4 | 96.0 | 95.2 | >100 |
| SK-MEL-28 | 50.3 | >100 | 36.9 | >100 |
| SK-MEL-5 | 22.6 | >100 | 37.3 | >100 |
| UACC-257 | 1.43 | 19.4 | 6.28 | >100 |
| UACC62 | 23.4 | >100 | 27.7 | >100 |
| Ovarian Cancer | ||||
| IGR-OV1 | 2.59 | >100 | 3.26 | >100 |
| OVCAR-3 | 2.08 | 11.5 | 2.29 | 30.1 |
| OVCAR-4 | 5.52 | >100 | 7.13 | >100 |
| OVCAR-5 | 34.9 | >100 | 42.1 | >100 |
| OVCAR-8 | 1.35 | 17.2 | 3.52 | >100 |
| NCI/ADR-RES | 1.88 | 36.5 | 1.99 | >100 |
| SK-OV-3 | 30.1 | >100 | 45.5 | >100 |
| Renal Cancer | ||||
| 786-0 | 3.44 | 43.0 | 23.0 | >100 |
| A498 | 34.5 | >100 | >100 | >100 |
| ACHN | 20.4 | >100 | >100 | >100 |
| CAKI-1 | 1.98 | >100 | 53.9 | >100 |
| RXF 393 | 6.29 | >100 | 7.40 | >100 |
| SN12C | 5.94 | >100 | >100 | >100 |
| TK-10 | 4.11 | >100 | >100 | >100 |
| UO-31 | 4.15 | >100 | 83.2 | >100 |
| Prostate Cancer | ||||
| PC-3 | 4.27 | >100 | 46.9 | >100 |
| DU-145 | 3.76 | 74.6 | 21.4 | >100 |
| Breast Cancer | ||||
| MCF7 | 3.22 | >100 | 6.93 | >100 |
| MDA-MB-231/ATCC | 8.55 | >100 | 19.4 | >100 |
| HS 578T | 2.04 | >100 | 60.3 | >100 |
| BT-549 | 2.98 | 54.9 | 8.45 | 97.0 |
| T-47D | 13.5 | >100 | 32.0 | >100 |
| MDA-MB-468 | 2.29 | >100 | 11.6 | >100 |
NA: Not analyzed
a
GI50: 50% Growth inhibition, concentration of drug resulting in a 50% reduction in net protein increase compared with control cells.
b
LC50: Lethal concentration, concentration of drug lethal to 50% of cells.