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Aliphatic Substitution of o-Carboranyl Phenols Enhances Estrogen Receptor Beta Selectivity
http://hdl.handle.net/2297/37544
http://hdl.handle.net/2297/37544b298b558-171e-49ef-98ed-e4465abf82e8
| 名前 / ファイル | ライセンス | アクション |
|---|---|---|
PH-PR-OGAWA-A-386.pdf (2.1 MB)
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| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2017-10-04 | |||||
| タイトル | ||||||
| タイトル | Aliphatic Substitution of o-Carboranyl Phenols Enhances Estrogen Receptor Beta Selectivity | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| 著者 |
Ohta, Kiminori
× Ohta, Kiminori× Ogawa, Takumi× Kaise, Asako× Oda, Akifumi× Endo, Yasuyuki |
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| 書誌情報 |
Chemical and Pharmaceutical Bulletin 巻 62, 号 4, p. 386-391, 発行日 2014-01-01 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0009-2363 | |||||
| NCID | ||||||
| 収録物識別子タイプ | NCID | |||||
| 収録物識別子 | AA00602100 | |||||
| DOI | ||||||
| 関連タイプ | isIdenticalTo | |||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1248/cpb.c13-00796 | |||||
| 出版者 | ||||||
| 出版者 | 日本薬学会 = The Pharmaceutical Society of Japan | |||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | The two subtypes of estrogen receptor (ER), ERα and ERβ, differ greatly in expression pattern and biological functions, and ERβ-selective ligands candidates to treat immune-related disorders. ERβ-selective ligands have mostly been designed based the idea of introducing a substituent that interferes sterically with the ligand’s interaction with Met421 to selectively decrease the affinity for ERα (the equivalent residue in ERβ is Ile373). Therefore, we designed and synthesized a series of carboranyl phenol derivatives bearing an aliphatic substituent as candidate ERβ-selective ligands. Introduction of a longer aliphatic substituent into the carboranyl moiety enhanced the ERβ selectivity of o-carboranyl phenol derivatives 4, but not m-carboranyl bisphenol derivatives 5. Compound 4c showed 7.4-fold ERβ selectivity in ER-binding assay and exhibited moderate estrogenic activity in cell proliferation assay using MCF-7 cell line. | |||||
| 権利 | ||||||
| 権利情報 | Copyright © 2014 The Pharmaceutical Society of Japan | |||||
| 著者版フラグ | ||||||
| 出版タイプ | VoR | |||||
| 出版タイプResource | http://purl.org/coar/version/c_970fb48d4fbd8a85 | |||||
| 関連URI | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | http://ci.nii.ac.jp/naid/130003390780 | |||||
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| 識別子タイプ | URI | |||||
| 関連識別子 | https://www.jstage.jst.go.jp/browse/cpb | |||||
| 関連URI | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | http://www.pharm.or.jp/ | |||||
