Synthesis and receptor-binding examination of 16-hydroxymethyl-3,17-estradiol stereoisomers
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-...
Elmentve itt :
| Szerzők: | |
|---|---|
| Dokumentumtípus: | Cikk |
| Megjelent: |
2002
|
| Sorozat: | STEROIDS
67 No. 7 |
| Tárgyszavak: | |
| doi: | 10.1016/S0039-128X(02)00020-X |
| mtmt: | 3043120 |
| Online Access: | http://publicatio.bibl.u-szeged.hu/39777 |
| Tartalmi kivonat: | 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. © 2002 Elsevier Science Inc. All rights reserved. |
|---|---|
| Terjedelem/Fizikai jellemzők: | 671-678 |
| ISSN: | 0039-128X |