Table 1. PR Binding and Functional Activities of 6, 7a−c, and 8a−h^a.

				binding				functional
				PR	MR	AR	GR	PR		MR
cmpd	R1	R2	isomer	Ki (nM)	Ki (nM)	Ki (nM)	Ki (nM)	IC50(nM)	% Inhib	IC50 (nM)	% Inhib
6				478 ± 287	86.8 ± 49.6	68.9 ± 16.8	50.2 ± 19.4	3720 ± 563	86.5 ± 2.26	>10000	40.8 ± 3.39
7a		H		454 ± 188	0.640 ± 0.864	220 ± 97.7	6.39 ± 3.43	765 ± 171	91.7 ± 4.59	64.1 ± 25.8	76.3 ± 12.8
7b		F	S	464 ± 158	0.319 ± 0.156	211 ± 99.4	5.93 ± 4.18	715 ± 61.9	89.7 ± 9.38	27.2 ± 13.7	62.9 ± 11.5
7c		F	R	1230 ± 260	1.51 ± 0.856	676 ± 306	54.4 ± 8.33	2020 ± 155	94.5 ± 0.141	306 ± 53.3	87.0 ± 2.12
8a	Me	H		28.0 ± 10.7	>4170	>4020	>4290	485 ± 214	87.8 ± 3.70	>10000	−2.2
8b	Et	H		4.23 ± 1.95	1770 ± 640	2590	927 ± 93.8	12.6 ± 2.47	97.0 ± 3.28	>10000	23.8 ± 7.23
8c	iPr	H		0.795 ± 0.286	1490 ± 123	>3900	1530 ± 156	6.81 ± 1.11	96.2 ± 1.34	>10000	36.6 ± 9.12
8d	iPr	Me		0.298 ± 0.150	126 ± 12.1	403 ± 212	157 ± 15.2	3.38 ± 0.698	95.8 ± 4.03	>10000	56.0 ± 7.37
8e	iPr	OMe		1.45 ± 0.760	1390 ± 403	490 ± 172	977 ± 65.7	7.28 ± 1.06	97.4 ± 0.726	2420	35.8 ± 2.31
8f	iPr	F		0.214 ± 0.0924	849 ± 223	648	523 ± 148	2.29 ± 0.860	94.9 ± 4.74	8150	50.2 ± 11.9
8g	sBu		S	0.320 ± 0.227	1000 ± 155	1740 ± 795	1860 ± 552	3.89 ± 1.04	96.8 ± 1.03	9800	43.4 ± 9.22
8h	sBu		R	0.834 ± 0.339	1440 ± 223	2550 ± 666	780 ± 147	9.92 ± 1.88	96.2 ± 0.635	>10000	39.2 ± 6.79

^aExperimental values represent the average of at least duplicate determinations. Standard deviations are indicated by ± of the geometric mean.