Table 4.

Hormonal activity and the growth inhibition of mono- and bivalent OHT ligands (11–17, 19, and 20).

Entry	Ligand	Hormonal Activity (U2OS Cells) a				Growth inhibition
		ERα		ERβ		IC50 after 96h [μM]
		IA b [%]	CD c [%]	IA b [%]	CD c [%]	MCF7	MDA-MB-231
1.	11ZZ	−71	81	−91	79	0.11	>20
2.	12ZZ	−64	80	−89	78	0.07	1.84
3.	13ZZ	−83	51	−93	55	0.11	1.95
4.	14ZZ	−85	61	−96	59	0.06	1.23
5.	15ZZ	−95	15	−99	15	0.08	1.20
6.	16ZZ	−100	10	−99	9	0.10	0.69
7.	17ZZ	−100	9	−100	8	2.10	13.98
8.	19ZZ	−100	8	−100	7	0.01	0.32
9.	19 d	−99	8	−100	6	0.15	0.32
10.	20Z	−42	-	−77	-	0.37	2.17
11.	20E	-	-	-	-	0.40	1.94
12.	OHT e	5	110	−47	92	0.15	4.59

^aConcentration 10μM.

^bIntrinsic activity (IA).

^cCell density (CD).

^dCell assays were evaluated based on Z-Z:Z-E:E-E = 1:2:1 isomers.

^eThe concentration was 1μM.