کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1254175 | 971354 | 2014 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Synthesis of 11β-ether-17α-ethinyl-3,17β-estradiols with strong ER antagonist activities Synthesis of 11β-ether-17α-ethinyl-3,17β-estradiols with strong ER antagonist activities](/preview/png/1254175.png)
We have previously found that several families of nonpolar short chain 11β-ethers and esters of estradiol are selective estrogen receptor modulators (SERMs). Surprisingly, the transformation from potent estrogen to anti-estrogen occurs when the 11β-side chain is increased slightly in length from four to five non-hydrogen atoms. To generate strong antagonists for preclinical development, we have synthesized other similar ER ligands with 11β-ethers and with an additional ethinyl group at the 17α-position in order to slow metabolism of the steroidal moiety. Here we report the synthesis and biological activity of two such compounds (11β-i-PrO-propyl and 11β-t-BuO-propyl ethers) with extremely strong antagonist activities.
We report here the synthesis of 17α-ethinyl-E11-3,t-Buether and 17α-ethinyl-E11-3,i-Prether estradiols, and their extremely strong antagonist activities.Figure optionsDownload as PowerPoint slide
Journal: Chinese Chemical Letters - Volume 25, Issue 4, April 2014, Pages 567–570