{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Lv W"],"funding":["NIGMS NIH HHS"],"pagination":["4611-8"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC4043309"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["56(11)"],"pubmed_abstract":["The first synthesis of the tamoxifen metabolite norendoxifen is reported. This included syntheses of (E)-norendoxifen, (Z)-norendoxifen, and (E,Z)-norendoxifen isomers. (Z)-Norendoxifen displayed affinity for aromatase (Ki 442 nM), estrogen receptor-α (EC50 17 nM), and estrogen receptor-β (EC50 27.5 nM), while the corresponding values for (E)-norendoxifen were aromatase (Ki 48 nM), estrogen receptor-α (EC50 58.7 nM), and estrogen receptor-β (EC50 78.5 nM). Docking and energy minimization studies were performed with (E)-norendoxifen on aromatase, and the results provide a foundation for structure-based drug design. The oral pharmacokinetic parameters for (E,Z)-norendoxifen were determined in mice, and (Z)-norendoxifen was found to result in significantly higher plasma concentrations and exp"],"journal":["Journal of medicinal chemistry"],"pubmed_title":["Synthesis of mixed (E,Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities."],"pmcid":["PMC4043309"],"funding_grant_id":["T32 GM008425"],"pubmed_authors":["Liu J","Flockhart DA","Cushman M","Lv W","Lu D"],"additional_accession":[]},"is_claimable":false,"name":"Synthesis of mixed (E,Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities.","description":"The first synthesis of the tamoxifen metabolite norendoxifen is reported. This included syntheses of (E)-norendoxifen, (Z)-norendoxifen, and (E,Z)-norendoxifen isomers. (Z)-Norendoxifen displayed affinity for aromatase (Ki 442 nM), estrogen receptor-α (EC50 17 nM), and estrogen receptor-β (EC50 27.5 nM), while the corresponding values for (E)-norendoxifen were aromatase (Ki 48 nM), estrogen receptor-α (EC50 58.7 nM), and estrogen receptor-β (EC50 78.5 nM). Docking and energy minimization studies were performed with (E)-norendoxifen on aromatase, and the results provide a foundation for structure-based drug design. The oral pharmacokinetic parameters for (E,Z)-norendoxifen were determined in mice, and (Z)-norendoxifen was found to result in significantly higher plasma concentrations and exp","dates":{"release":"2013-01-01T00:00:00Z","publication":"2013 Jun","modification":"2025-04-19T15:57:25.492Z","creation":"2019-03-27T01:29:22Z"},"accession":"S-EPMC4043309","cross_references":{"pubmed":["23731360"],"doi":["10.1021/jm400364h"]}}