Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist

Journal of Medicinal Chemistry

Volumn 58, Issue 20, 2015, Pages 8128-8140

  De Savi, Chris ^a   Bradbury, Robert H ^a   Rabow, Alfred A ^a   Norman, Richard A ^a   De Almeida, Camila ^a   Andrews, David M ^a   Ballard, Peter ^a   Buttar, David ^a   Callis, Rowena J ^a   Currie, Gordon S ^a   Curwen, Jon O ^a   Davies, Chris D ^a   Donald, Craig S ^a   Feron, Lyman J L ^a   Gingell, Helen ^a   Glossop, Steven C ^a   Hayter, Barry R ^a   Hussain, Syeed ^a   Karoutchi, Galith ^a   Lamont, Scott G ^a   MacFaul, Philip ^a   Moss, Thomas A ^a   Pearson, Stuart E ^a   Tonge, Michael ^a   Walker, Graeme E ^a   Weir, Hazel M ^a   Wilson, Zena ^a   more..

^a ASTRAZENECA   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

3 [3,5 DIFLUORO 4 [2 (2 FLUORO 2 METHYLPROPYL) 3 METHYL 2,3,4,9 TETRAHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]PHENYL]ACRYLIC ACID; ESTROGEN RECEPTOR ANTAGONIST; FULVESTRANT; UNCLASSIFIED DRUG; ANTIESTROGEN; ANTINEOPLASTIC AGENT; AZD9496; CINNAMIC ACID DERIVATIVE; INDOLE DERIVATIVE; SELECTIVE ESTROGEN RECEPTOR MODULATOR;

ARTICLE; CRYSTAL STRUCTURE; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; FEMALE; HUMAN; HUMAN CELL; MALE; MOUSE; NONHUMAN; PHASE 1 CLINICAL TRIAL (TOPIC); RAT; RECEPTOR DOWN REGULATION; BREAST NEOPLASMS; CELL PROLIFERATION; CHEMISTRY; DOWN REGULATION; DRUG DESIGN; DRUG EFFECTS; INTRAMUSCULAR DRUG ADMINISTRATION; METABOLISM; SYNTHESIS; TUMOR CELL LINE; X RAY DIFFRACTION;

ANTINEOPLASTIC AGENTS; BREAST NEOPLASMS; CELL LINE, TUMOR; CELL PROLIFERATION; CINNAMATES; CLINICAL TRIALS, PHASE I AS TOPIC; DOWN-REGULATION; DRUG DESIGN; ESTROGEN ANTAGONISTS; ESTROGEN RECEPTOR MODULATORS; FEMALE; HUMANS; INDOLES; INJECTIONS, INTRAMUSCULAR; X-RAY DIFFRACTION;

EID: 84945381593     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b00984     Document Type: Article

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