Table 5.
In vitro antiproliferative activity of the novel furanylnicotinamidines against a panel of 60 cell lines at a five-dose level (National Cancer Institute, Bethesda, MD, USA)
| Cancer type/cell line | 4b | 4c | 4d | 4e | 4f | 4g |
|---|---|---|---|---|---|---|
| Leukemia | ||||||
| CCRF-CEM | 3.20 | 2.06 | 1.80 | 0.856 | 1.51 | 1.93 |
| HL-60 (TB) | 2.14 | 2.12 | 1.76 | 0.219 | 1.52 | 2.42 |
| K-562 | 3.97 | 1.32 | 0.541 | 0.314 | 0.934 | 1.50 |
| MOLT-4 | 4.40 | 1.74 | 1.59 | 0.681 | 1.89 | 2.46 |
| RPMI-8226 | 2.78 | 1.92 | 1.30 | 0.310 | 1.20 | 2.03 |
| SR | 3.11 | 1.73 | 0.378 | 0.275 | 1.32 | 1.78 |
| Non-small cell lung cancer | ||||||
| A549/ATCC | 5.10 | 1.86 | 1.89 | 1.06 | 1.50 | 1.90 |
| HOP-62 | 10.5 | 1.70 | 1.74 | 1.35 | 1.50 | 1.98 |
| HOP-92 | 1.31 | 1.42 | 1.27 | 0.401 | 0.579 | 1.56 |
| NCI-H226 | 12.9 | 1.81 | 1.88 | 1.52 | 1.40 | 2.13 |
| NCI-H23 | 11.6 | 1.90 | 1.77 | 1.40 | 1.76 | 1.96 |
| NCI-H322M | 6.00 | 1.60 | 1.44 | 0.838 | 1.73 | 1.74 |
| NCI-H460 | 3.69 | 1.63 | 1.35 | 0.293 | 1.61 | 1.90 |
| NCI-H522 | 6.80 | 1.73 | 1.84 | 1.61 | 1.51 | 1.98 |
| Colon cancer | ||||||
| Colo 205 | 1.82 | 1.62 | 1.04 | 0.201 | 0.817 | 2.01 |
| HCC-2998 | 2.45 | 1.69 | 1.07 | 0.212 | 1.22 | 1.92 |
| HCT-116 | 3.26 | 1.66 | 1.47 | 0.405 | 1.40 | 1.97 |
| HCT-15 | 4.62 | 1.84 | 1.36 | 0.486 | 1.30 | 1.80 |
| HT29 | 3.40 | 1.39 | 0.479 | 0.319 | 0.736 | 1.76 |
| KM12 | 4.41 | 1.78 | 1.43 | 0.388 | 1.69 | 1.85 |
| SW-620 | 4.05 | 1.67 | 0.774 | 0.492 | 1.61 | 1.78 |
| CNS cancer | ||||||
| SF-268 | 11.2 | 1.86 | 1.77 | 1.30 | 1.55 | 1.82 |
| SF-295 | NT | 1.86 | 2.00 | 1.79 | 1.54 | 1.92 |
| SF-539 | 4.74 | 1.55 | 1.54 | 1.19 | 1.41 | 1.76 |
| SNB-19 | 11.7 | 1.85 | 1.87 | 1.56 | 1.72 | 1.63 |
| SNB-75 | 10.5 | 1.48 | 1.59 | 1.35 | 1.24 | 1.64 |
| U251 | 4.70 | 1.62 | 1.53 | 1.28 | 1.49 | 1.76 |
| Melanoma | ||||||
| LOX IMVI | 2.58 | 1.63 | 1.53 | 0.306 | 1.48 | 1.77 |
| MALME-3M | 3.25 | 1.82 | 2.04 | 1.35 | 1.94 | 2.42 |
| M14 | 2.12 | 1.90 | 1.85 | 1.31 | 1.54 | 1.90 |
| MDA-MB-435 | 2.18 | 1.55 | 1.24 | 0.381 | 1.36 | 1.76 |
| SK-MEL-2 | 4.91 | 2.01 | 1.96 | 1.95 | 2.02 | 2.09 |
| SK-MEL-28 | 8.23 | 1.65 | 1.76 | 1.52 | 1.59 | 1.80 |
| SK-MEL-5 | 3.43 | 1.60 | 1.58 | 1.48 | 1.46 | 1.77 |
| UACC-257 | 2.18 | 1.76 | 1.77 | 1.31 | 1.71 | 1.84 |
| UACC-62 | 10.3 | 1.77 | 1.76 | 1.57 | 1.69 | 1.78 |
| Ovarian cancer | ||||||
| IGROV-1 | 5.29 | 1.81 | 1.89 | 1.50 | 1.70 | 2.09 |
| OVCAR-3 | 8.90 | 1.89 | 1.75 | 1.34 | 1.87 | 1.88 |
| OVCAR-4 | 10.4 | 1.74 | 1.56 | 1.17 | 1.40 | 1.90 |
| OVCAR-5 | 10.9 | 1.74 | 1.62 | 1.19 | 1.58 | 1.73 |
| OVCAR-8 | 11.3 | 1.71 | 1.74 | 1.67 | 1.70 | 1.88 |
| NCI/ADR-RES | 14.1 | 6.53 | 2.03 | 1.63 | 1.69 | 1.93 |
| SK-OV-3 | 10.2 | 1.91 | 1.88 | 1.53 | 1.40 | 1.95 |
| Renal cancer | ||||||
| 786-0 | 6.02 | 1.72 | 1.79 | 1.27 | 1.46 | 1.95 |
| A498 | 12.8 | 1.22 | 1.09 | 0.770 | 1.26 | 1.47 |
| ACHN | 6.56 | 1.71 | 1.75 | 1.23 | 1.66 | 1.81 |
| CAKI-1 | 6.79 | NT | NT | NT | 1.30 | 1.76 |
| RXF 393 | 7.01 | 1.60 | 1.58 | 1.16 | 1.19 | 1.73 |
| SN12C | 8.01 | 1.62 | 1.58 | 1.23 | 1.69 | 1.62 |
| TK-10 | 10.7 | 1.79 | 1.95 | 1.94 | 1.74 | 1.87 |
| UO-31 | 2.68 | 1.59 | 1.48 | 0.960 | 1.60 | 1.54 |
| Prostate cancer | ||||||
| PC-3 | 4.18 | 1.65 | 1.50 | 1.03 | 1.48 | 1.74 |
| DU-145 | 11.3 | 1.76 | 1.72 | 0.834 | 1.70 | 1.87 |
| Breast cancer | ||||||
| MCF-7 | 3.17 | 1.74 | 1.61 | 0.484 | 1.37 | 1.73 |
| MDA-MB-231/ATCC | 3.34 | 1.83 | 1.80 | 0.469 | NT | 1.65 |
| HS-578T | 10.9 | 1.66 | 1.90 | 1.31 | 1.57 | 1.87 |
| BT-549 | 10.7 | 1.78 | 1.80 | 1.56 | 1.40 | 1.89 |
| T-47D | 5.13 | 1.72 | 1.73 | 0.379 | NT | 2.18 |
| MDA-MB-468 | 2.04 | 1.51 | 1.39 | 0.507 | 1.37 | 1.69 |
Note: Data represent the compounds’ GI50 in μM against the tested cell lines.
Abbreviations: GI50, drug concentration that causes 50% inhibition of cell growth; NT, not tested; CNS, central nervous system.