Table 2.

Hormonal activity and the growth inhibition of mono- and bivalent DES ligands (1–7).

Entry	Ligand	Hormonal activity (U2OS Cells)a				Growth inhibition
		ERα		ERβ		IC50 after 96h [μM]
		IA b [%]	CD c [%]	IA b [%]	CD c [%]	MCF-7	MDA-MB-231
1.	1 d	49	93	50	96	7.3	5.4
2.	2 d	79	95	104	92	9.0	9.1
3.	3 d	81	93	89	91	5.1	5.6
4.	4 d	22	86	58	86	5.5	4.9
5.	5 d	22	78	32	77	1.8	1.2
6.	6 d	33	88	89	85	<0.63	>20
7,	6 e	−7	80	55	90	<0.63	>20
8.	7 f	90	93	95	92	6.5	5.6
9.	DES g	105	103	111	90	5.9	4.3

^aConcentration of 1–7 was 10μM.

^bIntrinsic activity (IA).

^cCell density (CD).

^dPure Z-Z isomer.

^ePure E-Z isomer.

^fThe bivalent DES ligand 7 was evaluated based on 60% E-E isomer.

^gThe concentration was 10nM.