Table 2. In vitro inhibitory effects of compounds 10a-l.

Comp.	clogP Ann 2005	aIC50 (μM) ChoKα1 purified	Antiproliferative activity bGI50 (μM)
			HeLa	HT−29	Jurkat	HL-60	RS4,11	MCF-7	PC-3	A549	MDA-MB-231
10a	−0.36	1.00 ± 0.01	0.079 ± 0.024	0.11 ± 0.01	0.12 ± 0.08	0.10 ± 0.04	0.045 ± 0.005	0.092 ± 0.019	0.051 ± 0.01	0.027 ± 0.010	0.10 ± 0.05
10b	0.36	9.56 ± 1.45	0.082 ± 0.041	4.3 ± 0.42	0.068 ± 0.016	0.042 ± 0.005	1.12 ± 0.22	0.17 ± 0.032	4.5 ± 1.1	2.3 ± 1.1	0.09 ± 0.02
10c	1.8	1.63 ± 0.14	5.6 ± 0.25	4.3 ± 1.1	7.3 ± 0.50	2.1 ± 0.6	2.7 ± 0.13	3.5 ± 0.72	3.1 ± 0.7	4.9 ± 0.7	2.2 ± 0.27
10d	−1.01	37.54 ± 4.45	16.9 ± 2.5	>100	>100	84.1 ± 7.4	37.5 ± 4.2	91.4 ± 7.6	94.3 ± 12.4	61.3 ± 16.7	74.3 ± 2.6
10e	−2.42	9.51 ± 1.14	>100	94.0 ± 4.2	>100	>100	66.0 ± 6.6	50.9 ± 11.7	48.0 ± 1.1	>100	63.2 ± 3.9
10f	3.02	6.85 ± 0.81	0.15 ± 0.031	0.12 ± 0.017	0.060 ± 0.002	0.063 ± 0.013	0.24 ± 0.05	0.17 ± 0.065	0.47 ± 0.12	0.21 ± 0.06	0.001 ± 0.001
10g	3.56	3.27 ± 0.66	0.25 ± 0.06	0.75 ± 0.12	0.098 ± 0.031	0.71 ± 0.24	0.15 ± 0.04	0.46 ± 0.063	0.26 ± 0.01	0.11 ± 0.018	0.19 ± 0.009
10h	3.82	2.79 ± 0.17	0.32 ± 0.062	0.35 ± 0.07	0.31 ± 0.07	0.92 ± 0.06	0.026 ± 0.006	0.32 ± 0.04	0.85 ± 0.32	0.18 ± 0.08	0.23 ± 0.04
10i	4.23	16.22 ± 0.44	1.5 ± 0.73	1.0 ± 0.15	0.76 ± 0.26	0.87 ± 0.28	0.50 ± 0.09	0.66 ± 0.07	0.72 ± 0.09	0.29 ± 0.10	0.15 ± 0.05
10j	2.27	1.66 ± 0.09	0.17 ± 0.084	0.15 ± 0.08	0.11 ± 0.026	0.42 ± 0.22	0.16 ± 0.012	0.11 ± 0.047	0.09 ± 0.04	0.30 ± 0.068	0.01 ± 0.005
10k	2.76	2.02 ± 0.08	0.26 ± 0.074	0.27 ± 0.05	0.072 ± 0.013	0.18 ± 0.06	0.036 ± 0.008	0.28 ± 0.09	0.11 ± 0.028	0.52 ± 0.02	0.061 ± 0.003
10l	2.36	0.92 ± 0.01	0.37 ± 0.18	0.56 ± 0.21	0.007 ± 0.003	0.16 ± 0.07	0.42 ± 0.14	0.022 ± 0.007	0.8 ± 0.2	0.14 ± 0.06	0.05 ± 0.02
MN58b	0.01	0.78 ± 0,03	1.9 ± 0.1	1.9 ± 0.4	0.35 ± 0.1	0.32 ± 0.03	1.0 ± 0.3	1.8 ± 0.06	n.d.	0.54 ± 0.2	0.31 ± 0.12
RSM932A	2.92	1.92 ± 0,06	0.83 ± 0.1	0.4 ± 0.2	0.41 ± 0.1	0.93 ± 0.1	0.17 ± 0.04	0.18 ± 0.10	n.d.	0.45 ± 0.09	0.17 ± 0.05

^aIC₅₀ = Compound concentration required to inhibit ChoKα1 enzyme by 50%.

^bGI₅₀ = Compound concentration required to inhibit tumor-cell proliferation by 50%.

Values are the mean ± SEM for three independent experiments. n.d. not determined.