438536-55-1Relevant 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)
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
Modification of estrone at the 6, 16, and 17 positions: Novel potent inhibitors of 17β-hydroxysteroid dehydrogenase type 1
Allan, Gillian M.,Lawrence, Harshani R.,Cornet, Josephine,Bubert, Christian,Fischer, Delphine S.,Vicker, Nigel,Smith, Andrew,Tutill, Helena J.,Purohit, Atul,Day, Joanna M.,Mahon, Mary F.,Reed, Michael J.,Potter, Barry V. L.
, p. 1325 - 1345 (2007/10/03)
The 17β-hydroxysteroid dehydrogenases (17β-HSDs) catalyze the interconversion between the oxidized and reduced forms of androgens and estrogens at the 17 position. The 17β-HSD type 1 enzyme (17β-HSD1) catalyzes the reduction of estrone to estradiol and is
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.
