Table 1.

Effects on ER binding and inhibition of MCF-7 proliferation for a series of raloxifene analogs

Compound	R	R′	ER RBA	MCF-7 Inhib. IC50 (nM)
17β-estradiol			1.00	NA
4-OH Tam			0.36	0.5
Raloxifene (1)	6-OH	OH	0.34	0.2
1a	None	OH	.003	35
1b	6-OMe	OH	.008	250
1c	7-OH	OH	.020	300
1d	5-OH	OH	0.1	100
1e	6-OH	H	.062	2.5
1f	None	H	.002	>100

NA, not applicable.