. 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 1.

Activity of 3–29 (mono-substituted phenyl B-ring) against KB and KB-VIN

	R				ED₅₀ (µM)^a		Selectivity
	2’	3’	4’	5’	KB	KB-VIN	KB/KB-VIN
2					>236.7	1.07	>221
3			Me		39.2	0.08	460
4			Et		21.9	0.07	320
5			Pr		>53	12.16	>4
6			iPr		8.13	1.08	3
7			Bu		110.7	36.95	3.0
8			tBu		29.3	17.4	2
9			CF₃		35.7	10.35	3.5
10			OH		20.6	20.6	1
11			OMe		17.7	0.68	26
12			OEt		>52.4	7.54	>7
13			OPr		>50.5	29.17	>2
14			OCF₃		36.49	9.95	4
15			SMe		>52.1	1.38	>38
16			Br		>48.1	15.70	3
17			F		33.0	1.85	18
18			CH₂Br		>46.5	27.91	>2
19			CH₂OMe		>52.4	3.40	15
20		Me			49.7	3.69	14
21		CF₃			35.7	5.42	6.6
22		OMe			13.3	1.22	11
23		OCF₃			>47.4	9.95	>5
24		F			>56.2	3.09	>18
25	Me				40.9	2.41	17
26	CF₃				45.6	43.10	1
27	OMe				40.8	3.26	13
28	F				>56.2	3.93	>14

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.