Table 2.

Growth inhibition (GI₅₀; µM)^b data for PTL (1), DMAPT (2) and carbamoylated MMB analogs 6a–6e against a panel of human cancer cell lines

Panel/cell line	1a	2a	6a	6b	6c	6d	6e
Leukemia	GI50	GI50	GI50	GI50	GI50	GI50	GI50
CCRF-CEM	7.94	1.99	0.68	2.49	2.65	3.03	0.62
HL-60(TB)	5.01	1.58	2.04	4.15	NDb	3.59	NDb
K-562	19.9	2.51	3.45	3.26	NDb	3.37	NDb
MOLT-4	15.8	3.16	2.05	3.48	5.54	5.00	2.32
RPMI-8226	7.94	2.51	1.98	8.71	8.20	5.72	2.57
SR	NDb	ND	1.38	10.2	4.10	3.65	2.36
Non-Small cell lung cancer
HOP-92	12.5	10.0	1.45	2.25	2.25	2.30	0.65
NCI-H522	5.01	2.51	1.25	1.78	1.64	2.13	1.26
Colon cancer
COLO 205	15.8	31.6	2.06	4.78	3.54	8.89	1.79
HCT-116	10.0	5.01	1.41	3.18	1.89	2.87	1.13
SW-620	15.8	3.98	1.46	3.46	3.13	3.48	1.12
CNS cancer
SF-539	19.9	2.51	1.98	15.0	5.77	14.4	1.76
SNB-75	50.1	NDb	6.13	18.0	3.78	19.5	1.71
Melanoma
LOX IMVI	7.94	10.0	2.23	7.88	4.96	4.84	1.95
MALME-3M	12.5	NDb	1.90	4.18	7.52	6.12	2.32
M14	NDb	15.8	2.84	9.65	5.58	7.97	1.59
MDA-MB-435	NDb	7.94	0.46	6.56	6.01	5.89	2.24
Ovarian cancer
IGROV1	19.9	19.9	2.31	4.09	14.4	3.49	3.66
OVCAR-3	19.9	12.5	1.69	8.41	NDb	6.20	NDb
Renal cancer
ACHN	NDb	15.8	1.79	3.80	2.75	3.74	1.75
CAKI-1	10.0	12.5	2.03	6.86	2.88	4.31	1.99
RXF 393	12.5	15.8	1.20	4.08	2.22	3.00	0.90
TK-10	NDb	3.16	2.60	3.11	3.78	3.93	2.51
Prostate Cancer
DU-145	NDb	5.01	2.44	7.42	4.59	3.74	3.49
Breast cancer
MCF7	15.8	5.01	1.62	3.91	2.85	3.54	1.33
BT-549	NDb	5.01	2.69	4.75	2.60	4.99	1.47
T-47D	NDb	39.8	3.07	4.86	6.19	6.32	2.23
MDA-MB-468	NDb	NDb	0.57	2.30	3.22	3.26	1.29

^aGI₅₀ values obtained from NCI database

^bGI₅₀, concentration of analog (µM) that halves cellular growth.

^cND, not determined.

GI₅₀ values < 1µM are bolded