438536-56-2Relevant academic research and scientific papers
Stereocontrolled synthesis of the four possible 3-methoxy and 3-benzyloxy-16-triazolyl-methyl-estra-17-ol hybrids and their antiproliferative activities
Kiss, Anita,W?lfling, János,Mernyák, Erzsébet,Frank, éva,Benke, Zsanett,Ashkan Senobar Tahaei, Seyyed,Zupkó, István,Mahó, Sándor,Schneider, Gyula
, (2019/09/30)
The four possible isomers of each of 3-methoxy- and 3-benzyloxyestra-1,3,5(10)-trien-17-ols (5–8 and 9–12) were converted through 16-p-tosyloxymethyl- or 16-bromomethyl derivatives into their 3-methoxy- and 3-benzyloxy-16-azidomethylestra(1,3,5(10)-triene
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.
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.
