Table 3.

Summary of IC₅₀ values of 6a–m: Yields; inhibition of coregulatory peptide SRC2-2 and TRα/TRβ binding; viability (LD₅₀ ) of U2OS and ARO cell in the presence of compounds.

				In vitro Potency			Cytotoxicity
Entry	R=	Compound	Yielda (%)	TRαb IC50 (μM)	TRβb IC50 (μM)	TRα: TRβ ratio	AROc LD50 (μM)	U2OSc LD50 (μM)
1	4- n-propylphenyl	6a	85	>100	100	-	20.2	43.9
2	4- n-butylphenyl	6b	86	71.0	66.0	1.1	9.9	25.6
3	4- n-pentylphenyl	6c	88	60.9	33.9	1.8	20.0	22.7
4	4- tert-pentylphenyl	6d	94	69.6	43.5	1.6	5.8	27.5
5	4-n-hexylphenyl	6e	89	45.2	18.6	2.4	29.5	18.8
6	4-n-heptylphenyl	6f	76	23.0	10.5	2.2	69.2	36.7
7	4-n-octylphenyl	6g	81	21.4	11.4	1.9	111	50.5
8	(trans) 4-tert-pentylcyclohexyl	6h	62	75.6	69.1	1.1	92.8	50.2
9	4-n-propylbenzoate	6i	75	>100	61.0	-	4.8	121
10	4-n-pentylbenzoate	6j	71	>100	55.8	-	21.2	36.5
11	2-n-hexylbenzoate	6k	85	39.1	8.2	4.8	14.6	19.4
12	4-n-butyramidophenyl	6l	73	>100	85.9	-	8.6	242
13	5,6,7,8-tetrahydronaphthyl	6m	77	85.3	69.8	1.2	54.7	101

^aIso lated yield;

^bvalues are means of two independent experiments done in quadruplicate; the general error limits are 10%;

^cvalues are means of two independent experiments done in triplicate; the general error limits are 10–15%. Actual error values for each measurement are omitted for clarity but are included in tables in the supplemental materials.