438536-67-5Relevant academic research and scientific papers
Neighboring group participation: Part 16. Stereoselective synthesis and receptor-binding examination of the four stereoisomers of 16-bromomethyl-3,17- estradiols
Szajli, Agota,Woelfling, Janos,Mernyak, Erzsebet,Minorics, Renata,Marki, Arpad,Falkay, George,Schneider, Gyula
, p. 141 - 153 (2007/10/03)
The four possible isomers of 3-benzyloxy-16-hydroxymethylestra-1,3,5(10)- trien-17-ol (1a-4a) with proven configurations were converted into the corresponding 3-benzyloxy-16-bromomethylestra-1,3,5(10)-triene-3,17-diols (5e-8e). Depending on the reaction c
Synthesis and receptor-binding examination of 16-hydroxymethyl-3,17-estradiol stereoisomers
Tapolcsanyi, Pal,Woelfling, Janos,Falkay, George,Marki, Arpad,Minorics, Renata,Schneider, Gyula
, p. 371 - 377 (2007/10/03)
The four 16-hydroxymethylestra-1,3,5(10)-triene-3,17-diol isomers were synthesized and tested in a radioligand-binding assay. The estrogen receptor recognizes these compounds, but their relative binding affinities are lower than 2.0% relative to that of the reference molecule estra-1,3,5(10)-triene-3,17β-diol. The affinities of the tested compounds for the androgen and progesterone receptors are very low (Ki> 100 μm and 1 μM, respectively). The prepared 16-hydroxymethylestra-1,3,5(10)-triene-3,17-diol isomers are therefore estrogen receptor-selective molecules.
Synthesis and receptor-binding examination of 16-hydroxymethyl-3,17-estradiol stereoisomers
Tapolcsányi, Pál,W?lfling, János,Falkay, George,Márki, árpád,Minorics, Renáta,Schneider, Gyula
, p. 671 - 678 (2007/10/03)
The four 16-hydroxymethylestra-1,3,5(10)-triene-3,17-diol isomers were synthesized and tested in a radioligand-binding assay. The estrogen receptor recognizes these compounds, but their relative binding affinities are lower than 2.0% relative to that of the reference molecule estra-1,3,5(10)-triene-3,17β-diol. The affinities of the tested compounds for the androgen and progesterone receptors are very low (Ki> 100 μm and 1 μM, respectively). The prepared 16-hydroxymethylestra-1,3,5(10)-triene-3,17-diol isomers are therefore estrogen receptor-selective molecules.
