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. Author manuscript; available in PMC: 2016 Mar 6.
Published in final edited form as: Eur J Med Chem. 2014 Dec 29;92:212–220. doi: 10.1016/j.ejmech.2014.12.050

Table 1.

Growth inhibition (GI50/μM)a data for (Z)-indol-2-yl (8, 11), (Z)-benzo[b]furan-2-yl (12, 13), and (Z)-benzo[d]thiazol-2-yl (15, 17) cyano combretastatin analogues

Panel/cell line 8 9 11 12 13 15 17

μM μM μM μM μM μM μM
Leukemia
CCRF-CEM 0.017 0.062 0.136 0.024 0.777 0.055 na
HL-60(TB) <0.01 0.034 0.031 <0.01 0.481 0.066 0.345
K-562 <0.01 0.039 0.039 <0.01 0.467 0.051 0.333
MOLT-4 0.023 0.084 0.274 0.047 0.548 9.20 3.38
RPMI-8226 <0.01 0.151 0.199 0.019 1.32 0.237 2.29
SR <0.01 0.042 na <0.01 0.470 0.107 0.402
Lung Cancer
A549/ATCC <0.01 0.114 0.076 <0.01 0.520 0.379 na
EKVX 1.16 0.307 na 0.059 na na na
HOP-62 <0.01 na 0.092 <0.01 2.29 1.93 3.35
HOP-92 <0.01 0.058 0.077 <0.01 1.13 nd 0.534
NCI-H226 <0.01 0.399 14.5 <0.01 34.5 0.844 4.11
NCI-H23 <0.01 0.236 0.246 <0.01 3.11 3.25 2.84
NCI-H322M nd 0.735 0.465 <0.01 6.18 2.29 >10.0
NCI-H460 <0.01 0.053 0.093 <0.01 0.472 0.336 2.86
NCI-H522 <0.01 0.049 0.033 <0.01 0.438 0.022 na
Colon Cancer
COLO 205 0.016 0.232 0.097 <0.01 0.404 0.036 0.574
HCC-2998 0.018 0.366 0.265 0.01 2.33 0.297 8.39
HCT-116 <0.01 0.044 0.047 <0.01 0.418 0.052 0.404
HCT-15 <0.01 0.048 0.089 <0.01 0.469 0.045 0.414
HT29 <0.01 0.048 0.048 <0.01 0.373 0.037 0.438
KM12 <0.01 0.076 0.047 <0.01 0.356 0.278 2.01
SW-620 <0.01 0.042 0.048 <0.01 0.388 0.038 0.343
CNS Cancer
SF-268 0.015 1.48 0.086 0.247 2.05 1.03 3.09
SF-295 <0.01 0.036 0.037 <0.01 0.708 0.508 2.46
SF-539 <0.01 0.047 0.039 <0.01 1.56 0.097 1.68
SNB-19 <0.01 0.189 0.085 <0.01 5.55 2.49 >10.0
SNB-75 <0.01 0.036 0.039 <0.01 1.78 0.145 2.13
U251 <0.01 0.075 0.044 <0.01 0.760 1.65 1.91
Melanoma
LOX IMVI <0.01 0.064 0.090 <0.01 0.930 0.073 1.84
MALME-3M 8.28 nd nd 59.9 0.629 0.515 0.699
M14 <0.01 0.039 0.056 <0.01 0.437 0.193 1.21
MDA-MB-435 <0.01 0.021 0.024 <0.01 0.229 0.021 0.199
SK-MEL-2 <0.01 0.312 0.528 <0.01 0.487 0.287 0.958
SK-MEL-28 na 1.94 0.161 <0.01 3.51 1.81 1.98
SK-MEL-5 <0.01 0.142 0.060 <0.01 0.564 0.100 1.37
UACC-257 1.06 27.0 0.062 63.2 18.0 >100 na
UACC-62 <0.01 0.038 0.058 <0.01 0.557 0.052 0.755
Ovarian Cancer
IGROV1 <0.01 0.482 0.183 0.022 1.27 1.27 0.706
OVCAR-3 <0.01 0.034 0.042 <0.01 0.279 0.031 0.285
OVCAR-4 15.2 0.735 0.672 0.039 7.19 3.86 >10.0
OVCAR-5 0.08 0.471 0.259 0.042 5.23 0.347 4.85
OVCAR-8 <0.01 0.326 0.124 <0.01 3.98 0.438 3.13
NCI/ADR-RES <0.01 0.040 0.073 <0.01 0.317 0.059 1.47
SK-OV-3 <0.01 0.394 0.087 <0.01 2.49 0.626 1.79
Renal Cancer
786-0 <0.01 0.602 0.137 <0.01 5.84 1.06 2.44
A498 <0.01 0.040 0.029 <0.01 0.540 0.198 0.417
ACHN <0.01 0.082 0.079 0.217 12.4 0.089 0.518
CAKI-1 <0.01 0.103 0.035 <0.01 0.492 0.047 0.482
RXF 393 <0.01 0.151 0.055 <0.01 1.30 0.148 0.551
SN12C <0.01 0.779 0.269 <0.01 0.956 0.515 4.68
TK-10 <0.01 5.56 20.1 73.6 2.28 0.063 2.78
UO-31 <0.01 0.071 0.201 2.29 3.79 0.083 0.679
Prostate Cancer
PC-3 <0.01 0.062 0.105 <0.01 2.41 0.341 2.74
DU-145 <0.01 0.206 0.207 <0.01 1.30 0.333 1.07
Breast Cancer
MCF7 0.016 0.289 0.039 0.023 0.446 0.034 0.399
MDA-MB-231/ATCC 0.014 0.291 0.294 0.028 1.21 0.992 6.74
HS 578T <0.01 0.133 0.092 <0.01 1.88 1.29 2.01
BT-549 <0.01 0.0978 0.109 0.029 0.950 12.2 3.45
T-47D 2.50 0.573 95.2 4.34 0.996 nd 1.18
MDA-MB-468 0.022 0.350 0.041 0.022 0.421 0.084 2.04

na: Not analyzed, nd: not determined,

a

GI50: 50% growth inhibition, concentration of drug resulting in a 50% reduction in net cell growth as compared to cell numbers on day 0.