Identification and structure–activity relationships of a novel series of estrogen receptor ligands based on 7-thiabicyclo [2.2. 1] hept-2-ene-7-oxide

…, Y Zheng, C Dong, JA Katzenellenbogen…

文献索引：Wang, Pengcheng; Min, Jian; Nwachukwu, Jerome C.; Cavett, Valerie; Carlson, Kathryn E.; Guo, Pu; Zhu, Manghong; Zheng, Yangfan; Dong, Chune; Katzenellenbogen, John A.; Nettles, Kendall W.; Zhou, Hai-Bing Journal of Medicinal Chemistry, 2012 , vol. 55, # 5 p. 2324 - 2341

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被引用次数: 17

摘要

To develop estrogen receptor (ER) ligands having novel structures and activities, we have explored compounds in which the central hydrophobic core has a more three-dimensional topology than typically found in estrogen ligands and thus exploits the unfilled space in the ligand-binding pocket. Here, we build upon our previous investigations of 7-oxabicyclo [2.2. 1] heptene core ligands, by replacing the oxygen bridge with a sulfoxide. These new 7- ...