Table 10.

Summary of the SAR Study to Compare the Pharmaceutical Properties of Indole UT-155 (Compound 8) Substituted with Class I—III Blocking Groups at the 2- and/or 3-Positions of the B-Ring

		B	X	Y	AR LBD Binding (Ki)	DMPK (half-life; T1/2)	EnzR antiandrogenic effect (IC50)
Class I	27	CH	carbazole		↓	↑↑	Equal or less
	34	CH	N	N	↓	↑↑	Equal or less
Class II	31	CH or N	CH	N- or C-substituted	Equal or less	↑	Equal or less
	32	CH	N	CH	Equal or less	↑↑	↑
Class III	35	CH or N	N	C-substituted	Equal or less	↑↑↑	↑↑