. 2011 Jul 17;2(9):678–681. doi: 10.1021/ml200093v

Table 1. Inhibition of 17β-HSD1 by Compounds 1–5.

graphic file with name ml-2011-00093v_0003.jpg

		inhibition (%)
compound no.	R	at 0.01 μM^a	at 0.1 μM^a	IC₅₀ (nM)^b
1	–OH	35	66	27 ± 4
2	–CH₂OH	14	37	ND
3	–CH₂Br	20	36	430 ± 99
4	–CH₂CH₂OH	7	17	ND
5	–CH₂CH₂Br	23	49	68 ± 6

Inhibition of the transformation of [¹⁴C]-E1 (60 nM) into [¹⁴C]-E2 by 17β-HSD1 in T-47D intact cells. The experiment was performed in triplicate (SD < ±5%). The inhibitors were tested at two concentrations of 0.01 and 0.1 μM.

Mean ± SD of an experiment performed in triplicate. ND, not determined.