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
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 m-carborane bisphenol structure as a pharmacophore for selective estrogen receptor modulators
掲載誌名 正式名:BIOORGANIC&MEDICINAL CHEMISTRY LETTERS
ISSNコード:0960894X
出版社 PERGAMON-ELSEVIER SCIENCE LTD
巻・号・頁 16(15),pp.3943-3946
著者・共著者 Takumi Ogawa,Kiminori Ohta,Tomohiro Yoshimi,Hiroto Yamazaki,Tomoharu Suzuki,Shigeru Ohta,Yasuyuki Endo
発行年月 2006/08
概要 A series of m-carborane derivatives was prepared based upon the structures of antiestrogenic drugs and their activities were evaluated by estrogen receptor alpha (ER alpha) binding assay and transactivation assay using human breast cancer cell line, MCF-7 cells. The m-carborane bisphenol 5 exhibited about a thousand times more potent ER agonistic activity than the o-carborane bisphenol 11. The m-carborane bisphenol structure appears to be a favorable hydrophobic pharmacophore for the development of novel selective estrogen receptor modulators (SERMs). (c) 2006 Elsevier Ltd. All rights reserved.
DOI 10.1016/j.bmcl.2006.05.032
PMID 16735120