Estrogen receptor binding characteristics of 1,11 beta-ethanoestradiol: effect of a 1,11 beta-bridge on steroidal estrogen.
Estrogen receptor binding characteristics of 1,11 beta-ethanoestradiol: effect of a 1,11 beta-bridge on steroidal estrogen.
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1,11 β-乙醇雌二醇的雌激素受体结合特征：1,11 β-桥对类固醇雌激素的影响。
DOI：
10.1016/0960-0760(90)90341-h
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发表时间：
1990
期刊：
影响因子：
--
通讯作者：
Hanson,RN
中科院分区：
文献类型：
--
作者：
Napolitano,E;Fiaschi,R;Hanson,RN
As part of an ongoing program to develop high affinity estrogenic ligands we have synthesized the 11β-vinyl, 11β-ethyl- and 1,11β-ethanoestradiols. Because the 1,11β-ethanoestradiol had not been previously reported in the literature, the investigation of its receptor binding characteristics would provide valuable insight into the effect of 1/11β-substitution. The data obtained in this study indicate that although significant estrogen receptor affinity is present for the 1,11β-ethano derivative, the RBA values, 5–22.4%, were far less than those observed (5–300-fold less) for the corresponding 11β-ethyl and 11β-vinyl estradiols and less than those for the 1-methyl and 11β-methyl estradiols. These results suggest that the orientation that the 11β-substituent must occupy is directed away from the A-ring and that substituents in the 1–11 pocket produce a detrimental effect on receptor interactions.
