Novel nonsteroidal selective estrogen receptor modulators. Carbon and heteroatom replacement of oxygen in the ethoxypiperidine region of raloxifene

…, JP Sluka, KM Duke, AW Glasebrook

Index: Schmid, Christopher R.; Sluka, James P.; Duke, Kristen M.; Glasebrook, Andrew W. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 4 p. 523 - 528

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Citation Number: 14

Abstract

Compounds were synthesized where oxygen in the ethoxypiperidine region of raloxifene is replaced with carbon, sulfur, or nitrogen linkages. Thia-and aza-substituted compounds were prepared by novel methodology. The compounds were evaluated in vitro as selective estrogen receptor modulators (SERMs). Calculations suggested the compounds exhibit an ER-α binding affinity/conformational energy relationship.