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オガワ タクミ
Ogawa Takumi
小川 匠 所属 鶴見大学 歯学部 歯学科 クラウンブリッジ補綴学 鶴見大学 歯学部 歯学科 歯科医学教育学 職種 教授 |
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| 論文種別 | 【査読あり】 研究論文（学術雑誌） |
| 言語種別 | 英語 |
| 査読の有無 | 査読あり |
| 表題 | Synthesis and biological evaluation of p-carborane bisphenols and their derivatives: Structure-activity relationship for estrogenic activity |
| 掲載誌名 | 正式名：BIOORGANIC&MEDICINAL CHEMISTRY |
| 出版社 | PERGAMON-ELSEVIER SCIENCE LTD |
| 巻・号・頁 | 17(3),pp.1109-1117 |
| 著者・共著者 | Takumi Ogawa,Kiminori Ohta,Toru Iijima,Tomoharu Suzuki,Shigeru Ohta,Yasuyuki Endo |
| 発行年月 | 2009/02 |
| 概要 | p-Carborane bisphenols and their derivatives were prepared and evaluated for binding affinity to estrogen receptor alpha. Their estrogenic activity was evaluated by means of transcriptional assay and cell proliferation assay using MCF-7 cell lines. 1,12-Bis(4-hydroxyphenyl)-1,12-dicarba-closo-dodecaborane 4a showed potent estrogenic activity, approaching that of 17 beta-estradiol, in transactivation assay. The activity of isomers 5a and 6a was drastically affected by the change in the position of one of the hydroxyl groups; 6a (ortho-OH in one ring) was about 1000 times less potent than 4a. Modification of this hydroxyl group with alkyl groups decreased the estrogenic activity in all isomers. Compound 4a also showed potent MCF-7 cell proliferation-enhancing activity. (C) 2008 Elsevier Ltd. All rights reserved. |
| DOI | 10.1016/j.bmc.2008.12.044 |