Table 3.

IC₅₀ ± SD (n = 3) values (μM) for CETZOLE-1, SAHA and the designed library of electrophilic heterocycles on HCT-116 and NCI-H522 cell lines.

	IC50 (μM)		Fold Change*
Compound	HCT-116	NCI-H522
CETZOLE-1	>40	3.99 ± 0.33	> 10.02
SAHA	1.31 ± 0.08	1.72 ± 0.28	0.76
8	8.39 ± 0.53	0.67 ± 0.07	12.52
9	4.88 ± 1.28	0.66 ± 0.05	7.39
10	15.88 ± 1.02	0.54 ± 0.09	29.40
16	23.18 ± 1.96	0.37 ± 0.03	62.64
30	>40	>40	N.A
29	>40	>40	N.A
28	>40	>40	N.A
27	>40	>40	N.A
32	>40	>40	N.A
34	>40	>40	N.A
36	>40	>40	N.A
38	>40	>40	N.A
31	17.51 ± 1.59	1.02 ± 0.05	17.16
37	>40	>40	N.A
33	>40	11.7 ± 2.08	3.41
35	>40	>40	N.A
39	9.5 ± 1.04	2.34 ± 0.27	4.05
40	>40	>40	N.A
41	>40	>40	N.A
42	>40	12.2 ± 2.26	> 3.27
43	19.36 ± 3.68	8.14 ± 1.10	2.37
44	11.61 ± 1.11	1.26 ± 0.08	9.12
45	19.61 ± 1.95	0.86 ± 0.06	22.80
47	24.96 ± 3.74	2.17 ± 0.13	11.50
46	>40	>40	N.A
48	>40	5.65 ± 0.58	> 7.07
24	>40	>40	N.A
22	>40	2.67 ± 0.34	> 14.98
18	>40	>40	N.A
20	>40	>40	N.A
51	>40	>40	N.A
49	>40	>40	N.A
57	>40	3.53 ± 0.40	11.33
56	>40	>40	N.A
1	>40	8.40 ± 1.81	> 4.76
2	5.61 ± 0.52	0.89 ± 0.07	6.30
60	>40	>40	N.A
61	>40	>40	N.A
58	>40	>40	N.A
59	>40	>40	N.A

^*As fold change is the ratio of IC₅₀ (HCT-116)/ IC₅₀ (NCI-H522).