Table 3.

Compound 1, synthetic analogs of library 11 and SAR.

Entry	Compound ID	R1	R2	IC50 (μM) CT-L a
13	1			0.60 ± 0.18 (n=27)
14	11a			1.08 ± 0.33 (n=4)
15	11b			0.43 ± 0.12 (n=4)
16	11c			2.53 ± 0.95 (n=5)
17	11d			0.94 ± 0.26 (n=8)
18	11e			1.12 ± 0.33 (n=5)
19	11f			1.41 ± 0.19 (n=2)
20	11g			1.07 ± 0.05 (n=4)
21	11h			0.51 ± 0.16 (n=6)
22	11i			0.45 ± 0.15 (n=4)
23	11j			6.20 ± 1.1 (n=2)
24	11k			8.50 ± 0.60 (n=2)
25	11l			11.20 ± 2.1 (n=3)
26	11m			0.31 ± 0.08 (n=4)
27	11n			0.97 ± 0.15 (n=2)
28	11o			No inhibition @ 10 μM
29	11p			No inhibition @ 10 μM
30	11q			No inhibition @ 10 μM
31	11r			No inhibition @ 10 μM
32	11s			10.09 ± 1.63(n=3)
33	11t			No inhibition @ 10 μM
34	11u			0.98 ± 0.50 (n=3)
35	11v			10.12 ± 4.5 (n=3)
36	11w			3.75 ± 1.47 (n=6)
37	11x			0.22 ± 0.084 (n=6)
38	11y			0.37 ± 0.05 (n=4)
39	11z			4.0 ± 0.90 (n=3)
40	11aa			0.26 ± 0.05 (n=6)
41	11ab			0.099 ± 0.032 (n=14)
42	11ac			2.71 ± 0.56 (n=5)
43	11ad			0.027 ± 0.014 (n=20)
44	11ae			0.039 ± 0.01 (n=7)
45	11af			0.120 ± 0.04 (n=3)
46	11ag			0.43 ± 0.04 (n=3)
47	11ah			1.36 ± 0.18 (n=3)
48	11ai			0.44 ± 0.07 (n=3)
49	11aj			46.49 ± 1.23(n=3)
50	11ak			0.140 ± 0.05 (n=3)
51	11al			0.032 ± 0.003 (n=3)
52	11am			0.105 ± 0.031 (n=3)
53	11an			0.107 ± 0.013 (n=3)
54	11ao			1.27 ± 0.22 (n=3)
55	11ap			0.273 ± 0.10 (n=3)
56	11aq			No inhibition @ 10 μM
57	11ar			1.93 ± 0.61 (n=4)
58	11as			0.14 ± 0.064 (n=4)

^aIC₅₀ values are given as the average of 2 or more determinations; n = number of determinations.