Table 1.

Antitumor analysis and comparison of compounds 9 and 11 with compound 2

		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

^aThe activity improvement factor is obtained from 10^Δ2-x, where x is the identifying value for compound 9 or 11. An activity improvement factor of 1.0 means no difference in activity.

^bNon-small cell lung.

^cCentral 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.