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. Author manuscript; available in PMC: 2022 Nov 15.
Published in final edited form as: Eur J Med Chem. 2021 Jun 30;224:113675. doi: 10.1016/j.ejmech.2021.113675

Table 1.

Antitumor activity (GI50/μM)a data for the substituted benzyl and phenethyl carbamate derivatives of MMB (7a-c, 7h, 7i and 7k) from the NCI-five dose human cancer cell panel assay

1b 7a 7b 7c 7h 7i 7k

Panel/cell line GI50 GI50 GI50 GI50 GI50 GI50 GI50
Leukemia
CCRF-CEM 7.94 0.47 0.26 0.48 0.34 1.98 0.27
HL-60(TB) 5.01 1.69 0.26 1.61 1.36 2.34 1.06
K-562 19.9 1.57 0.37 0.82 0.61 3.08 0.53
MOLT-4 15.8 2.00 0.28 2.53 2.09 2.61 1.69
RPMI-8226 7.94 1.8G 0.26 1.77 0.91 2.85 0.62
SR nd 0.32 0.30 0.67 0.51 2.07 0.43
Lung Cancer
A549/ATCC nd 2.58 2.43 3.07 7.28 13.2 2.59
EKVX nd 2.06 1.29 1.98 1.78 7.45 1.54
HOP-62 nd 3.06 4.81 3.69 4.39 12.2 1.99
HOP-92 12.5 1.42 0.24 1.49 1.84 1.99 1.28
NCI-H226 nd 2.02 0.48 2.11 1.57 4.11 1.72
NCI-H23 nd 1.84 0.55 1.74 1.86 4.34 1.72
NCI-H322M nd 4.72 nd nd nd 12.6 nd
NCI-H460 nd 3.01 2.74 3.73 3.94 12.2 2.06
NCI-H522 5.01 0.34 0.17 0.35 1.02 1.82 1.16
Colon Cancer
COLO 205 15.8 1.35 0.24 1.75 1.55 1.94 1.82
HCC-2998 nd 1.94 0.51 1.82 1.68 2.48 1.71
HCT-116 10.0 0.77 0.19 0.54 0.71 1.34 0.47
HCT-15 nd 0.77 0.24 1.04 1.02 1.74 1.01
HT29 nd 1.20 0.26 1.22 1.14 2.15 1.32
KM12 nd 2.80 2.35 3.53 4.27 8.36 1.95
SW-620 15.8 1.12 0.22 0.76 0.52 2.51 0.71
CNS Cancer
SF-268 nd 2.46 0.75 2.20 1.78 10.6 1.56
SF-295 nd 7.78 10.8 5.02 7.26 13.5 3.81
SF-539 19.9 1.54 0.32 1.53 1.49 1.79 1.46
SNB-19 nd 5.32 0.70 1.57 1.43 8.65 1.39
SNB-75 50.1 1.99 0.74 2.44 1.47 4.09 1.20
U251 nd 3.16 0.96 2.20 nd 11.1 1.40
Melanoma
LOX IMVI 7.94 0.54 0.27 1.43 1.34 1.38 1.18
MALME-3M 12.5 1.86 0.20 1.89 1.84 2.44 2.09
M14 nd 1.64 0.19 1.10 1.29 1.98 1.26
MDA-MB-435 nd 1.99 0.42 1.70 1.58 3.53 1.58
SK-MEL-2 nd 1.66 1.18 1.71 1.73 8.97 1.58
SK-MEL-28 nd 1.47 0.27 1.52 1.35 1.99 1.47
SK-MEL-5 nd 3.48 1.20 2.86 1.84 6.23 1.71
UACC-257 nd 1.54 0.32 1.48 1.53 2.49 1.63
UACC-62 nd 0.66 nd nd nd 1.25 nd
Ovarian Cancer
IGROV1 19.9 2.12 0.29 1.57 1.26 2.61 1.08
OVCAR-3 19.9 1.01 0.28 0.87 0.99 2.19 0.98
OVCAR-4 nd 1.70 0.49 1.78 1.78 3.41 1.56
OVCAR-5 nd 1.82 1.46 2.29 2.25 2.65 1.96
OVCAR-8 nd 1.60 0.49 2.45 2.26 2.77 1.49
NCI/ADR-RES nd 2.98 1.79 2.26 2.95 10.0 2.26
Renal Cancer
786-0 nd 1.70 0.18 1.16 1.37 1.76 1.04
A498 nd 2.11 0.72 3.23 2.35 4.52 2.07
ACHN nd 1.29 0.27 1.27 1.12 1.72 1.32
CAKI-1 10.0 1.59 0.31 1.38 1.19 2.52 1.42
RXF 393 12.5 0.68 0.19 1.04 0.67 1.55 1.20
TK-10 nd 1.66 0.35 1.79 1.61 2.73 1.73
UO-31 nd 1.51 0.16 1.68 1.39 1.76 1.55
Prostate Cancer
PC-3 nd 2.72 1.87 3.13 2.30 8.08 1.73
DU-145 nd 0.72 0.37 0.69 0.89 1.92 0.77
Breast Cancer
MCF7 15.8 0.58 0.27 0.49 0.49 1.89 0.41
MDA-MB-231 nd 1.61 0.62 1.47 1.56 2.02 1.42
HS 578T nd 4.12 0.79 3.40 3.43 13.8 2.41
BT-549 nd 1.57 0.20 1.25 1.51 2.12 1.10
T-47D nd 1.85 0.34 2.01 1.61 2.47 1.38
MDA-MB-468 nd 0.58 0.24 0.66 0.85 1.55 0.84
Average GI50 14.96 1.92 0.86 1.80 1.82 4.4 1.44

GI50 values <1μM are bolded; nd: not determined;

a

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

b

5-dose NCI cancer cell screening data for PTL (1).[10]