Table 3. ERα Activity of Compounds 5a–g.

				EC50 (nM)
compd	R1	R2	n	ERα bindinga	ERα agonismb
5a	NH2	H	1	238	1430
5b	CO2H	H	1	i.a.	i.a.
5c	CO2Me	H	1	i.a.	i.a.
5d	H	OH	1	7790	>3000
5e	OH	OH	1	>10 000	>10 000
5f	H	H	1	490	900
5g	OH	H	2	2600	9500

^aERα LiSA assay.

^b(ERE)₇-TK-Luc reporter assay in HepG2 cells. i.a. = inactive at 10 μM. All data in triplicate ±15%.