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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 2.

Growth inhibition (GI50/μM)a data for (Z)-indole-3-yl (2124) and (Z)-benzo[b]furan-3-yl (25) cyanocombretastatin analogues

Panel/cell line 21 22 23 24 25

μM μM μM μM μM
Leukemia
CCRF-CEM 0.058 2.74 0.042 0.064 1.41
HL-60(TB) 0.048 4.57 0.031 0.059 1.03
K-562 0.040 1.65 0.043 0.044 0.513
MOLT-4 0.131 3.99 0.049 0.198 3.82
RPMI-8226 0.231 3.96 0.065 0.241 2.47
SR 0.022 1.45 0.033 0.027 0.681
Lung Cancer
A549/ATCC 0.078 5.16 0.061 0.086 0.665
EKVX 0.596 18.5 0.478 0.485 na
HOP-62 0.082 8.69 0.273 0.133 6.98
HOP-92 1.01 5.26 0.068 0.083 3.02
NCI-H226 0.194 20.9 8.18 0.170 6.20
NCI-H23 0.133 7.19 0.256 0.101 4.58
NCI-H322M nd 24.3 nd 0.044 19.1
NCI-H460 0.041 4.51 0.039 0.037 0.839
NCI-H522 0.037 3.05 0.027 0.086 0.261
Colon Cancer
COLO 205 0.474 5.31 0.047 0.051 0.449
HCC-2998 0.107 12.6 0.207 0.119 4.13
HCT-116 0.048 35.5 0.042 0.045 0.517
HCT-15 0.051 3.70 0.053 0.068 0.492
HT29 0.038 3.32 0.038 0.038 0.394
KM12 0.043 4.04 0.040 0.044 0.586
SW-620 0.047 3.53 0.044 0.046 0.504
CNS Cancer
SF-268 2.54 18.9 0.078 2.14 4.79
SF-295 0.042 4.92 0.045 0.042 0.446
SF-539 0.099 8.42 0.052 0.071 0.442
SNB-19 0.076 24.2 0.062 0.089 3.63
SNB-75 0.042 6.04 0.034 0.043 0.769
U251 0.050 4.97 0.045 0.050 0.605
Melanoma
LOX IMVI 0.075 5.32 0.078 0.074 0.993
MALME-3M 12.5 9.91 nd 5.85 0.868
M14 0.053 3.75 0.042 0.052 0.667
MDA-MB-435 0.024 3.95 0.020 0.027 0.278
SK-MEL-2 na 4.70 0.051 na 0.304
SK-MEL-28 0.090 6.25 0.081 0.092 1.61
SK-MEL-5 0.042 4.27 0.048 0.036 0.336
UACC-257 11.3 11.9 nd 10.7 nd
UACC-62 0.048 6.98 0.049 0.059 0.519
Ovarian Cancer
IGROV1 0.417 21.0 0.347 0.379 3.06
OVCAR-3 0.033 5.68 0.031 0.034 0.277
OVCAR-4 0.338 22.1 3.52 1.35 2.61
OVCAR-5 10.6 >100 0.197 0.516 3.33
OVCAR-8 0.121 7.38 0.103 0.148 2.90
NCI/ADR-RES 0.039 1.70 0.033 0.037 0.382
SK-OV-3 0.051 11.9 0.117 0.056 1.71
Renal Cancer
786-0 0.090 14.1 0.077 0.085 6.11
A498 0.035 3.36 0.035 0.025 0.458
ACHN 1.76 23.7 nd 1.66 1.94
CAKI-1 0.058 4.34 0.035 0.072 0.650
RXF 393 0.036 4.48 0.083 0.033 0.496
SN12C 0.699 8.10 0.077 0.715 2.17
TK-10 11.1 13.2 10.3 20.1 2.10
UO-31 1.41 14.3 0.663 1.26 2.89
Prostate Cancer
PC-3 0.054 7.85 0.075 0.054 1.84
DU-145 0.132 22.6 0.130 0.153 1.88
Breast Cancer
MCF7 0.034 3.10 0.041 0.036 0.376
MDA-MB-231/ATCC 0.245 7.18 0.644 0.299 1.71
HS 578T 0.131 12.9 0.611 0.124 2.03
BT-549 1.94 5.38 0.049 0.348 0.927
T-47D 0.058 6.83 nd 0.065 0.811
MDA-MB-468 0.041 na 0.051 0.035 0.237

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.