Table 2.
Anti‐proliferative activities of 82, 91 and 95 against a panel of human cancer cell lines
Anti‐proliferative activity, GI50 (μM)a | |||||
---|---|---|---|---|---|
Cancer type | Cell line | 82 | 91 | 95 | PD0332991 |
Breast | MCF7 | 0.660 ± 0.190 | 1.390 ± 0.190 | 0.290 ± 0.092 | 0.557 ± 0.040 |
T47D | – | 0.839 ± 0.092 | – | 1.180 ± 0.071 | |
Colorectal | COLO205 | 3.610 ± 0.311 | 2.220 ± 0.247 | 2.130 ± 0.481 | 1.170 ± 0.085 |
HCT116 | 7.470 ± 0.148 | 3.610 ± 0.113 | 1.240 ± 0.007 | 1.290 ± 0.262 | |
HT29 | 5.610 ± 0.877 | 3.750 ± 0.410 | 1.390 ± 0.041 | 1.400 ± 0.113 | |
Leukaemia | MOLM13 | 0.408 ± 0.018 | 0.076 ± 0.006 | 0.098 ± 0.008 | 0.061 ± 0.003 |
NB4 | 0.511 ± 0.100 | 0.431 ± 0.096 | 0.120 ± 0.006 | 0.033 ± 0.067 | |
U937 | 4.920 ± 0.014 | 2.860 ± 0.276 | 1.370 ± 0.849 | 1.080 ± 0.085 | |
Melanoma | M229 | 2.210 ± 0.290 | 3.380 ± 0.573 | 2.830 ± 0.601 | 1.220 ± 0.431 |
M238 | 2.420 ± 0.014 | 2.750 ± 0.445 | 1.090 ± 0.007 | 1.970 ± 0.184 | |
M238R1 | 1.950 ± 0.092 | 1.180 ± 0.028 | 4.690 ± 1.287 | 1.620 ± 0.368 | |
M249 | 5.570 ± 0.134 | 0.550 ± 0.092 | 0.960 ± 0.071 | 1.990 ± 0.368 | |
M249R | 10.50 ± 0.919 | 0.313 ± 0.049 | 1.100 ± 0.003 | 2.960 ± 0.156 | |
Ovarian | A2780 | 0.552 ± 0.098 | 0.028 ± 0.002 | 0.041 ± 0.004 | 0.045 ± 0.013 |
Prostate | PC3 | 0.230 ± 0.106 | 0.220 ± 0.049 | 1.240 ± 0.375 | 0.740 ± 0.212 |
DU145 | >10 | 5.657 ± 0.312 | 9.405 ± 0.421 | 8.596 ± 0.106 | |
Untransformed | |||||
Embryonic lung fibroblasts | WI‐38 | >10 | >10 | >10 | >10 |
MRC‐5 | >10 | 8.320 ± 0.305 | 8.110 ± 0.028 | >10 |
Anti‐proliferative activity was determined by 72 h resazurin and MTT assays using leukaemia and solid cancer cell lines respectively. GI50 is the compound concentration required to inhibit 50% of cell growth. The data given are derived from at least two replicates and are presented as mean ± SEM.