Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERα-selective tetrahydroisoquinoline ligands

Journal of Medicinal Chemistry

Volumn 48, Issue 2, 2005, Pages 364-379

  Renaud, Johanne ^a,b   Bischoff, Serge François ^a,c   Buhl, Thomas ^a,b   Floersheim, Philipp ^a,c   Fournier, Brigitte ^a,b   Geiser, Martin ^a,d   Halleux, Christine ^a,b   Kallen, Joerg ^a,d   Keller, Hansjoerg ^a,b   Ramage, Paul ^a,d  

^a NOVARTIS PHARMA AG   (Switzerland)

^b Arthr/Bone Metab Therapeutic Area ^*  (Switzerland)

^c Nervous System Therapeutic Area   (Switzerland)

^d Central Technologies

Author keywords

[No Author keywords available]

Indexed keywords

1 [4 (OCTAHYDROPYRIDO[1,2 A]PYRAZIN 2 YL)PHENYL] 2 PHENYL 1,2,3,4 TETRAHYDROISOQUINOLIN 6 OL; ESTRADIOL; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; LASOFOXIFENE; PIPERAZINE DERIVATIVE; PIPERIDINE DERIVATIVE; RALOXIFENE; SELECTIVE ESTROGEN RECEPTOR MODULATOR; TETRAHYDROISOQUINOLINE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; BREAST CANCER; CELL STRAIN MCF 7; CHIRALITY; CROSS COUPLING REACTION; CRYSTAL STRUCTURE; DRUG BIOAVAILABILITY; DRUG CONFORMATION; DRUG SAFETY; DRUG STRUCTURE; DRUG SYNTHESIS; ESTROGEN RESPONSIVE ELEMENT; FEMALE; HORMONE SUBSTITUTION; HUMAN; HUMAN CELL; LIGAND BINDING; MOLECULAR MODEL; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

ANIMALS; BIOLOGICAL AVAILABILITY; CELL LINE, TUMOR; CRYSTALLOGRAPHY, X-RAY; DRUG SCREENING ASSAYS, ANTITUMOR; ESTROGEN RECEPTOR ALPHA; FEMALE; HUMANS; INHIBITORY CONCENTRATION 50; ISOQUINOLINES; LIGANDS; MODELS, MOLECULAR; PIPERAZINES; PIPERIDINES; RADIOLIGAND ASSAY; RATS; SELECTIVE ESTROGEN RECEPTOR MODULATORS; STRUCTURE-ACTIVITY RELATIONSHIP; TETRAHYDROISOQUINOLINES;

EID: 19944431090     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm040858p     Document Type: Article

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