Fluorine-substituted cyclofenil derivatives as estrogen receptor ligands: synthesis and structure-affinity relationship study of potential positron emission tomography …

…, KE Carlson, JA Katzenellenbogen

Index: Seo, Jai Woong; Comninos, John S.; Chi, Dae Yoon; Kim, Dong Wook; Carlson, Kathryn E.; Katzenellenbogen, John A. Journal of Medicinal Chemistry, 2006 , vol. 49, # 8 p. 2496 - 2511

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Citation Number: 43

Abstract

In a search for estrogen receptor (ER) ligands to be radiolabeled with fluorine-18 for imaging of ER-positive breast tumors with positron emission tomography (PET), we investigated cyclofenil analogues substituted at the C3 or C4 position of the cyclohexyl group. McMurry coupling of 4, 4'-dihydroxybenzophenone with various ketones produced key cyclofenil intermediates, from which C3 and C4 substituents containing alkyl and various oxygen or ...