Table 1.

Effects of tether length and composition on transcription and cytotoxicity in transfected PC-3 cells^a

Cmpd	L	IC50 SRE.Lb (µ M)	% inh SRE.Lb (10, 100 µM)	% inh pRL-TKc (10, 100 µM)	% inh WST-1d (10, 100 µM)
1	-OCH(CH3)-	1.5	74, ND	48, ND	44, ND
5a	-OCH2-	4.7	71, 100	53, 89	42, 91
4a	-CH2CH2-	38	38, 64	0, 22	0, 10
4b	-CH2-	33	45, 85	15, 25	0, 30
4c	-CH2CH2CH2-	21	37, 79	5, 42	0, 12
4d	-CH2CH2CH2CH2-	>100

^aFor assay descriptions, see Ref 20. All values are mean of ≥ 3 experiments, each run in triplicate.

^bInhibition of Rho-pathway selective serum response element-luciferase reporter.

^cInhibition of control pRL-thymidine kinase Renilla luciferase reporter.

^dInhibition of mitochondrial metabolism of WST-1.