کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1363527 | 981514 | 2009 | 10 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Synthesis and evaluation of aryl-substituted diarylpropionitriles, selective ligands for estrogen receptor β, as positron-emission tomographic imaging agents Synthesis and evaluation of aryl-substituted diarylpropionitriles, selective ligands for estrogen receptor β, as positron-emission tomographic imaging agents](/preview/png/1363527.png)
We have investigated halogen-substituted non-steroidal estrogens with selective binding affinity for the estrogen receptor β (ERβ that might be used for imaging the levels of this ER-subtype in breast tumors by positron emission tomography (PET). Based on diarylpropionitrile (DPN, 1a), a compound previously reported that has a 72-fold binding selectivity for ERβ, we developed a series of DPN analogs having methyl-, hydroxyl-, and halogen substituents, including fluoroethyl and fluoropropyl groups. In competitive radiometric binding assays with [3H]estradiol, all of these DPN analogs showed high ERβ/ERα selectivity; while the selectivity varied, in some cases it reached nearly 300-fold (RBA: ERα, 0.023%; ERβ, 6.25%). The absolute ERβ binding affinities, however, were not sufficient to merit further consideration for developing these ligands as PET imaging agents.
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Journal: Bioorganic & Medicinal Chemistry - Volume 17, Issue 9, 1 May 2009, Pages 3479–3488