کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1366579 | 981595 | 2007 | 5 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Synthesis, characterization, and estrogen receptor binding affinity of flavone-, indole-, and furan-estradiol conjugates Synthesis, characterization, and estrogen receptor binding affinity of flavone-, indole-, and furan-estradiol conjugates](/preview/png/1366579.png)
Different flavone-, indole-, and furan-17β-estradiol conjugates, linked via alkyl spacer chains extending from the 17α-position of the estradiol moiety, were synthesized by Pd-catalyzed cross-coupling reactions. Structures were assigned based on spectroscopic data. In vitro competitive binding assays for the estrogen receptor (α-ER), using [3H]estradiol (RBA = 100) as a competitor, revealed that a two-carbon alkyl linker combined with a flavone conjugate provided the highest binding affinity (RBA ∼ 9), warranting further studies on their potential use as selective estrogen-receptor modulators (SERMs) for hormone-replacement therapies.
Flavone-, indole-, and furan-17β-estradiol conjugates with 2–8 carbon linker chains extending from the 17α-position of the estradiol were synthesized by Pd-catalyzed cross-coupling reactions. In vitro competitive binding assays for the estrogen receptor revealed that a two-carbon alkynyl linker combined with a flavone conjugate provided the highest binding affinity.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 11, 1 June 2007, Pages 3212–3216