. Author manuscript; available in PMC: 2011 Sep 23.

Published in final edited form as: J Med Chem. 2010 Sep 23;53(18):6699–6705. doi: 10.1021/jm100846r

Table 2.

Activity of 30–56 (multi-substituted phenyl B-ring) against KB and KB-VIN

	R				ED₅₀ (µM)^a		Selectivity
	2’	3’	4’	5’	KB	KB-VIN	KB/KB-VIN
29	Me		Me		41.2	8.52	5
30		Me	Me		35.5	0.71	50
31		Cl	Me		39.0	2.15	18
32		F	Me		28.1	2.95	10
33	Me		Me	Me	8.2	4.37	2
34	Me		OMe		20.9	2.62	8
35		Me	OMe		28.5	0.10	273
36		OMe	OMe		14.7	1.00	15
37		F	OMe		26.7	0.10	250
38		Cl	OMe		24.9	1.37	18
39	Me	Me	OMe		5.43	0.28	20
40	Me		OMe	Me	36.6	7.58	5
41	OMe	OMe	OMe		9.4	1.57	6
42		OMe	OMe	OMe	46.7	5.6	8
43		Cl	OMe	OMe	21.8	8.40	3
44		OH	OH		10.0	5.41	2
45	Me	Me	OH		6.5	2.75	2
46		Me	OH	Me	18.3	8.90	2
47	Me	Me			3.1	0.85	4
48	Me			Me	14.5	3.41	4
49		Me		Me	45.5	0.45	100
50	OMe	OMe			35.2	4.02	9
51	OMe			OMe	8.8	2.51	4
52		OMe		OMe	45.2	3.27	14
53	OEt	OEt			44.6	31.69	1.4
54	F			Me	47.3	3.24	15
55		Me	F		40.5	1.62	24

Cytotoxicity as ED₅₀ values for each cell line, the concentration of compound that caused 50% reduction in absorbance at 562 nm relative to untreated cells using the sulforhodamine B assay.