Table 1.
Average log(GI50) values |
comparison with 9 |
comparison with 11 |
|||||||
---|---|---|---|---|---|---|---|---|---|
Tumor cell lines | 2 | 9 | 10 | 11 | Δ2–9 | activity improvement factora |
Δ2–11 | activity improvement factora |
|
Leukemia | CCRF-CEM | −7.55 | −7.61 | −6.81 | −7.62 | 0.06 | 1.14 | 0.07 | 1.16 |
HL-60(TB) | −7.27 | −7.62 | −6.87 | −7.76 | 0.35 | 2.24 | 0.49 | 3.09 | |
K-562 | −7.61 | −7.76 | −6.82 | −7.71 | 0.15 | 1.40 | 0.10 | 1.26 | |
MOLT-4 | −7.32 | −7.70 | −6.86 | −7.56 | 0.39 | 2.43 | 0.25 | 1.76 | |
RPMI-8226 | −7.93 | −7.79 | −6.86 | −7.80 | −0.14 | 0.73 | −0.13 | 0.75 | |
SR | −7.85 | −7.89 | −7.08 | −7.93 | 0.04 | 1.11 | 0.08 | 1.22 | |
NSCLb | A549/ATCCC | −7.38 | −7.69 | −6.77 | −7.61 | 0.31 | 2.04 | 0.23 | 1.68 |
EKVX | −6.87 | −7.07 | −6.66 | −7.04 | 0.21 | 1.60 | 0.17 | 1.48 | |
HOP-62 | −7.25 | −7.61 | −6.86 | −7.78 | 0.36 | 2.26 | 0.53 | 3.39 | |
HOP-92 | −7.52 | −7.57 | −6.89 | −7.70 | 0.04 | 1.11 | 0.18 | 1.50 | |
NCI-H226 | −7.34 | −7.69 | −6.84 | −7.46 | 0.36 | 2.26 | 0.12 | 1.32 | |
NCI-H23 | −7.38 | −7.65 | −6.95 | −7.83 | 0.27 | 1.86 | 0.45 | 2.79 | |
NCI-H322M | −7.24 | −7.63 | −6.86 | −7.80 | 0.39 | 2.43 | 0.56 | 3.63 | |
NCI-H460 | −7.67 | −7.75 | −6.84 | −7.75 | 0.08 | 1.19 | 0.08 | 1.19 | |
NCI-H522 | −7.85 | −7.75 | −6.57 | −7.70 | −0.10 | 0.79 | −0.15 | 0.70 | |
Colon | COLO 205 | −7.31 | −7.67 | −7.08 | −7.52 | 0.35 | 2.26 | 0.21 | 1.60 |
HCC-2998 | −7.21 | −7.79 | −7.00 | −7.89 | 0.58 | 3.76 | 0.68 | 4.79 | |
HCT-116 | −7.71 | −7.78 | −6.85 | −7.83 | 0.07 | 1.17 | 0.11 | 1.30 | |
HCT-15 | −5.98 | −5.98 | −5.95 | −6.74 | 0.00 | 1.00 | 0.77 | 5.82 | |
HT29 | −7.12 | −7.67 | −6.80 | −7.61 | 0.55 | 3.55 | 0.49 | 3.13 | |
KM12 | −7.53 | −7.75 | −6.89 | −7.89 | 0.22 | 1.66 | 0.37 | 2.32 | |
SW-620 | −7.53 | −7.65 | −6.88 | −7.62 | 0.12 | 1.30 | 0.09 | 1.22 | |
CNSc | SF-268 | −7.51 | −7.65 | −6.83 | −7.73 | 0.15 | 1.40 | 0.22 | 1.66 |
SF-295 | −7.40 | −7.70 | −6.89 | −7.77 | 0.30 | 2.00 | 0.37 | 2.32 | |
SF-539 | −7.48 | −7.60 | −6.93 | −7.68 | 0.12 | 1.30 | 0.20 | 1.58 | |
SNB-19 | −7.36 | −7.55 | −6.84 | −7.77 | 0.19 | 1.55 | 0.41 | 2.57 | |
SNB-75 | −7.52 | −7.49 | −7.13 | −7.96 | −0.03 | 0.93 | 0.44 | 2.75 | |
U251 | −7.63 | −7.73 | −6.84 | −7.76 | 0.10 | 1.26 | 0.13 | 1.35 | |
Melanoma | LOX IMVI | −7.69 | −7.78 | −6.83 | −7.87 | 0.09 | 1.23 | 0.18 | 1.51 |
MALME-3M | −7.62 | −7.71 | −6.95 | −7.46 | 0.09 | 1.23 | −0.16 | 0.69 | |
M14 | −7.00 | −7.34 | −6.94 | −7.44 | 0.34 | 2.19 | 0.44 | 2.75 | |
MDA-MB-435 | −7.37 | −7.63 | −6.98 | −7.60 | 0.26 | 1.82 | 0.23 | 1.70 | |
SK-MEL2 | −7.47 | −7.56 | −6.71 | −7.82 | 0.09 | 1.23 | 0.35 | 2.24 | |
SK-MEL28 | −7.56 | −7.73 | −6.94 | −7.68 | 0.16 | 1.46 | 0.11 | 1.30 | |
SK-MEL-5 | −7.56 | −7.77 | −7.02 | −7.65 | 0.21 | 1.62 | 0.10 | 1.24 | |
UACC-257 | −7.16 | −7.38 | −6.71 | −7.23 | 0.22 | 1.66 | 0.07 | 1.17 | |
UACC-62 | −7.91 | −7.92 | −7.05 | −7.87 | 0.01 | 1.02 | −0.04 | 0.91 | |
Ovarian | IGROV1 | −7.12 | −7.98 | −6.65 | −7.63 | 0.86 | 7.16 | 0.51 | 3.24 |
OVCAR-3 | −7.16 | −7.71 | −6.84 | −7.70 | 0.55 | 3.51 | 0.54 | 3.43 | |
OVCAR-4 | −6.68 | −7.25 | −6.78 | −7.14 | 0.57 | 3.76 | 0.46 | 2.88 | |
OVCAR-5 | −7.10 | −7.40 | −6.82 | −7.51 | 0.30 | 1.97 | 0.41 | 2.57 | |
OVCAR-8 | −7.27 | −7.45 | −6.70 | −7.59 | 0.18 | 1.51 | 0.32 | 2.11 | |
NCI/ADR-RES | −5.11 | −4.30 | −4.87 | −5.78 | −0.81 | 0.15 | 0.67 | 4.68 | |
SK-OV-3 | −6.99 | −7.58 | −6.74 | −7.60 | 0.59 | 3.85 | 0.61 | 4.03 | |
Renal | 786-0 | −7.21 | −7.49 | −6.78 | −7.60 | 0.28 | 1.88 | 0.39 | 2.43 |
A498 | −7.49 | −7.84 | −6.95 | −7.32 | 0.35 | 2.24 | −0.16 | 0.68 | |
ACHN | −6.81 | −7.46 | −6.59 | −7.13 | 0.65 | 4.47 | 0.32 | 2.09 | |
CAKI-1 | −6.64 | −6.86 | −6.44 | −6.90 | 0.22 | 1.64 | 0.26 | 1.82 | |
RXF 393 | −7.59 | −7.53 | −7.66 | −7.87 | −0.06 | 0.86 | 0.28 | 1.91 | |
SN12C | −7.45 | −7.68 | −6.82 | −7.61 | 0.23 | 1.70 | 0.16 | 1.45 | |
TK-10 | −6.89 | −7.28 | −6.82 | −7.07 | 0.39 | 2.45 | 0.17 | 1.50 | |
UO-31 | −6.78 | −7.16 | −6.44 | −6.90 | 0.38 | 2.40 | 0.11 | 1.30 | |
Prostate | PC-3 | −7.00 | −7.67 | −6.83 | −7.64 | 0.67 | 4.62 | 0.64 | 4.37 |
DU-145 | −7.04 | −7.69 | −6.74 | −7.60 | 0.65 | 4.47 | 0.56 | 3.63 | |
Breast | MCF7 | −7.89 | −7.86 | −6.84 | −7.70 | −0.04 | 0.92 | −0.19 | 0.65 |
MDA-MB-231/ATCC | −6.88 | −7.32 | −6.62 | −7.18 | 0.44 | 2.75 | 0.30 | 2.00 | |
HS578T | −7.55 | −7.79 | −6.83 | −7.79 | 0.25 | 1.76 | 0.25 | 1.76 | |
BT-549 | −7.77 | −7.74 | −7.06 | −7.87 | −0.03 | 0.94 | 0.10 | 1.26 | |
T-47D | −7.35 | −7.59 | −6.91 | −7.47 | 0.24 | 1.74 | 0.12 | 1.32 | |
MDA-MB-468 | −7.30 | −7.47 | −7.03 | −7.63 | 0.17 | 1.48 | 0.33 | 2.14 | |
Mean log(GI50) | −7.30 | −7.52 | −6.80 | −7.55 | |||||
Mean GI50 (nM) | 51 | 30 | 158 | 28 |
The activity improvement factor is obtained from 10Δ2-x, where x is the identifying value for compound 9 or 11. An activity improvement factor of 1.0 means no difference in activity.
Non-small cell lung.
Central nervous system. Numbers shadowed in different greys mean an increase of antitumor activity (from light to dark grey) for the corresponding compound in relation to compound 2 and the tumor cell line tested.