Table 2.

Structure–activity relationship exploration and metabolic stability in liver microsomes of alkyl, carboxyl, and carboxamide substituents.

Compound	Y[a]	PR transactivation assay		Metabolic stability assay
		IC50 [nm]	Efficacy [%]	F max Human [%]	F max Rat [%]
4	H	0.17	90	79	88
5		0.01	99	31	54
6		0.01	100	28	53
7		0.05	100	66	61
8		0.04	100	8	47
9		25	99	98	n.d.[b]
10		14	99	n.d.[b]	n.d.[b]
11		0.09	100	97	97
12		0.90	100	75	95
13		1.4	99	39	60

[a] Substituent at the 4′ position of the 11β‐phenyl ring. [b] Not determined.