Table 4.
Cytotoxic activities (GI50, TGI and LC50) of compounds 11, 13, 14, and 15 against 60 human cancer cell lines in vitro. Values where GI50 < 100 nM or TGI/LC50 < 10 μM are highlighted in bold.
| 11 | 13 | 14 | 15 | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Leukemia | GI50 (μM) | TGI (μM) | LC50 (μM) | GI50 (μM) | TGI (μM) | LC50 (μM) | GI50 (μM) | TGI (μM) | LC50 (μM) | GI50 (μM) | TGI (μM) | LC50 (μM) |
| CCRF-CEM | 19.6 | 64.1 | >100 | 2.25 | >100 | >100 | 3.57 | >100 | >100 | 0.4 | >100 | >100 |
| HL-60 (TB) | >100 | >100 | >100 | 2.16 | >100 | >100 | 2.79 | 34.9 | >100 | 0.32 | >100 | >100 |
| K-562 | 5.03 | >100 | >100 | 0.47 | >100 | >100 | 0.59 | >100 | >100 | 0.28 | >100 | >100 |
| MOLT-4 | 5.46 | >100 | >100 | 2.66 | >100 | >100 | 4.08 | >100 | >100 | 0.56 | >100 | >100 |
| RPMI-8226 | 7.03 | >100 | >100 | 2.87 | >100 | >100 | 4.51 | >100 | >100 | 0.39 | >100 | >100 |
| SR | 4.44 | >100 | >100 | 0.40 | >100 | >100 | 0.53 | >100 | >100 | 0.25 | >100 | >100 |
| Non-Small-Cell Lung Cancer | ||||||||||||
| A549/ATCC | 1.71 | 3.75 | 8.23 | 2.11 | >100 | >100 | 5.16 | >100 | >100 | 0.72 | 94.7 | >100 |
| EKVX | 9.37 | 62.4 | >100 | 3.35 | >100 | >100 | 4.83 | 5.6 | >100 | 0.64 | >100 | >100 |
| HOP-62 | 2.62 | 8.19 | 35.7 | 3.23 | >100 | >100 | 3.55 | >100 | >100 | 0.56 | 21.7 | >100 |
| HOP-92 | 2.13 | 6.71 | 90.1 | 3.51 | >100 | >100 | 3.76 | 23.7 | >100 | 1.95 | 21.3 | >100 |
| NCI-H226 | 2.28 | 6.48 | >100 | 4.11 | >100 | >100 | 4.38 | 28.8 | >100 | 1.25 | 71.2 | >100 |
| NCI-H23 | 3.07 | 11.6 | 49.6 | 4.75 | >100 | >100 | 4.22 | 52.6 | >100 | 0.93 | 28 | >100 |
| NCI-H233M | >100 | >100 | >100 | n.d. | >100 | >100 | 5.98 | 27.4 | >100 | 0.52 | 49.2 | >100 |
| NCI-H460 | 2.59 | 6.68 | >100 | 2.89 | >100 | >100 | 3.37 | 12 | >100 | 0.36 | 12.5 | 93.6 |
| NCI-H552 | 6.77 | >100 | >100 | 1.79 | >100 | >100 | 2.67 | 27.1 | >100 | 0.24 | 21.5 | >100 |
| Colon Cancer | ||||||||||||
| COLO 205 | 8.04 | >100 | >100 | n.d. | >100 | >100 | 9.92 | >100 | >100 | 5.13 | >100 | >100 |
| HCC-2998 | >100 | >100 | >100 | n.d. | >100 | >100 | 6.07 | >100 | >100 | 1.94 | 29.1 | >100 |
| HCT-116 | 1.83 | 4.06 | 8.99 | 3.36 | >100 | >100 | 3.31 | >100 | >100 | 0.42 | >100 | >100 |
| HCT-15 | 3.28 | 21.1 | >100 | 0.68 | >100 | >100 | 1.65 | >100 | >100 | 0.06 | >100 | >100 |
| HT29 | 6.48 | >100 | >100 | 3.25 | >100 | >100 | 3.64 | >100 | >100 | 3.18 | 13.6 | >100 |
| KM12 | 8.17 | >100 | >100 | 2.38 | >100 | >100 | 2.76 | 55.2 | >100 | 0.2 | 15.3 | >100 |
| SW-620 | 3.56 | >100 | >100 | 0.73 | >100 | >100 | 2.5 | >100 | >100 | 0.35 | >100 | >100 |
| CNS Cancer | ||||||||||||
| SF-268 | 4.94 | 26.1 | >100 | 4.49 | >100 | >100 | 4.71 | 48.2 | >100 | 0.6 | 31 | >100 |
| SF-295 | 2.94 | 9.13 | 32.6 | 2.36 | >100 | >100 | 2.98 | 13.2 | 43.2 | 0.3 | 3.79 | 99.3 |
| SF-539 | 2.21 | 5.50 | 20.5 | 3.10 | >100 | >100 | 2.73 | 10.4 | 36.3 | 0.28 | 1.25 | 18.2 |
| SNB-19 | 4.17 | 21.7 | >100 | 2.98 | >100 | >100 | 2.99 | 15.7 | >100 | 0.48 | 20.5 | >100 |
| SNB-75 | 1.65 | 4.41 | 14.9 | n.d. | n.d. | n.d. | 2.39 | 8.5 | 59.6 | 0.17 | 0.64 | 44.2 |
| U251 | 2.01 | 4.45 | 9.84 | 3.04 | >100 | >100 | 3.63 | >100 | >100 | 0.41 | 16 | >100 |
| Melanoma | ||||||||||||
| LOX IMVI | 4.74 | 22.6 | >100 | 2.75 | >100 | >100 | 3.41 | >100 | >100 | 0.51 | >100 | >100 |
| MALME-3M | 3.17 | >100 | >100 | 2.43 | >100 | >100 | 2.13 | 11.9 | 57.6 | 0.63 | >100 | >100 |
| M14 | 27.6 | >100 | >100 | 2.38 | >100 | >100 | n.d. | n.d. | n.d. | 0.5 | >100 | >100 |
| MDA-MB-435 | 6.03 | >100 | >100 | 0.31 | >100 | >100 | 0.36 | 2.03 | >100 | 0.1 | 0.33 | >100 |
| SK-MEL-2 | 15.1 | 38.0 | 95.7 | 2.44 | >100 | >100 | 5.62 | 34.2 | >100 | 0.79 | 78.5 | >100 |
| SK-MEL-28 | n.d. | >100 | >100 | n.d. | >100 | >100 | 3.64 | 25.8 | >100 | 2.78 | >100 | >100 |
| SK-MEL-5 | 4.10 | 25.4 | >100 | 2.39 | >100 | >100 | 3 | 9.58 | 42.4 | 0.17 | 3.25 | >100 |
| UACC-257 | >100 | >100 | >100 | n.d. | >100 | >100 | 6.72 | 63.5 | >100 | >100 | >100 | >100 |
| UACC-62 | 6.58 | >100 | >100 | 2.89 | >100 | >100 | 2.39 | 12.8 | 61.1 | 0.3 | 14 | >100 |
| Ovarian Cancer | ||||||||||||
| IGROV1 | 3.61 | 15.9 | 86.3 | 3.20 | >100 | >100 | 2.98 | 18.5 | 94.5 | 0.23 | 25.5 | >100 |
| OVCAR-3 | 2.12 | 4.12 | 7.99 | 1.72 | 4.91 | >100 | 2.05 | 5.2 | 21.5 | 0.22 | 1.59 | >100 |
| OVCAR-4 | 2.45 | 5.94 | >100 | 3.38 | >100 | >100 | 4.49 | 47.8 | >100 | 8.9 | 41.5 | >100 |
| OVCAR-5 | 7.18 | >100 | >100 | >100 | >100 | >100 | 4.82 | 27.3 | >100 | 0.55 | 22.6 | >100 |
| OVCAR-8 | 3.67 | 3.21 | >100 | 3.61 | >100 | >100 | 4.65 | >100 | >100 | 0.54 | 17.1 | >100 |
| NCI/ADR-RES | 3.45 | 22.5 | >100 | 1.28 | >100 | >100 | 1.99 | 18 | >100 | 0.45 | 26.7 | >100 |
| SK-OV-3 | 14.9 | 50.7 | >100 | 5.56 | >100 | >100 | 3.57 | 17.9 | 96.4 | 0.4 | 14.1 | 74.3 |
| Renal Cancer | ||||||||||||
| 786-0 | 2.01 | 4.15 | 8.56 | 4.42 | >100 | >100 | 5.15 | 27 | >100 | 1.04 | 20.7 | 91.4 |
| A498 | 4.05 | 17.8 | 65.2 | 2.48 | n.d. | >100 | 3.08 | 13.9 | 65.8 | 0.34 | 14 | 75.9 |
| ACHN | 2.91 | 9.63 | 60.5 | 4.25 | >100 | >100 | 3.38 | 13 | 41.5 | 0.59 | >100 | >100 |
| CAKI-1 | 3.74 | 18.7 | 78.2 | 2.77 | >100 | >100 | 4.24 | 20.3 | 73.5 | 0.28 | 15 | 80.3 |
| RXF 393 | 2.21 | 6.34 | 30.1 | 2.45 | 9.56 | >100 | 1.74 | 5.34 | 28.1 | 0.21 | 0.79 | 38.1 |
| SN12C | 4.02 | >100 | >100 | 4.05 | >100 | >100 | 3.5 | 17.6 | 94.5 | 0.79 | 60.4 | >100 |
| TK-10 | 1.88 | 3.71 | 7.30 | n.d. | >100 | >100 | 10.4 | 28.6 | 78.5 | 10.7 | 79.4 | >100 |
| UO-31 | 2.44 | n.d. | >100 | n.d. | >100 | >100 | 3.57 | 21.5 | >100 | 0.62 | 22.9 | 98.3 |
| Prostate Cancer | ||||||||||||
| PC-3 | 5.75 | >100 | >100 | 3.30 | >100 | >100 | 5.13 | 41.6 | >100 | 0.52 | 27.2 | >100 |
| DU-145 | 7.97 | >100 | >100 | 3.78 | >100 | >100 | 4.35 | 16.4 | 51.7 | 0.4 | 2.14 | >100 |
| Breast Cancer | ||||||||||||
| MCF7 | 7.40 | >100 | >100 | 0.82 | >100 | >100 | 1.63 | >100 | >100 | 0.03 | >100 | >100 |
| MDA-MB-231/ATCC | 2.04 | 5.26 | 22.6 | 3.58 | >100 | >100 | 3.96 | 18.4 | 68.2 | 1.05 | 22.4 | >100 |
| HS 578T | 2.60 | 7.80 | >100 | 2.46 | >100 | >100 | 3.61 | 32.6 | >100 | 0.3 | 2.45 | >100 |
| BT-549 | 5.19 | 38.9 | >100 | 4.03 | >100 | >100 | 4.96 | 37.2 | >100 | 0.77 | >100 | >100 |
| T-47D | 2.54 | n.d. | >100 | 2.96 | >100 | >100 | 4.36 | >100 | >100 | 0.21 | >100 | >100 |
| MDA-MB-468 | 4.95 | 35.8 | >100 | 0.38 | 3.03 | >100 | 1.5 | 6.42 | >100 | 0.13 | 0.64 | >100 |