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ID: ALA1135087
Journal: Bioorg Med Chem Lett
Title: Synthesis and biological evaluation of novel thio-substituted chromanes as high-affinity partial agonists for the estrogen receptor.
Authors: Christiansen LB, Wenckens M, Bury PS, Gissel B, Hansen BS, Thorpe SM, Jacobsen P, Kanstrup A, Jørgensen AS, Naerum L, Wassermann K.
Abstract: Synthesis of (+/-)-cis-7-hydroxy-3-phenyl-4-(4-(2-piperidinoethanethio)phenyl)chromane (13) and (+/-)-cis-7-hydroxy-3-phenyl-4-(4-(2-pyrrolidinoethanethio)phenyl)chromane (15) is presented. These compounds are representatives of a novel class of compounds with high in vitro binding affinity for the estrogen receptor (IC(50)=7-10 nM), and very low in vitro uterotrophic activity (max stim.=5-17% rel to moxestrol; EC(50)=0.5-1.8 nM).
CiteXplore: 11738564