Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core

Bioorganic and Medicinal Chemistry

Volumn 16, Issue 7, 2008, Pages 3744-3758

  Bonger, Kimberly M ^a   van den Berg, Richard J B H N ^a   Knijnenburg, Annemiek D ^a   Heitman, Laura H ^a   IJzerman, Ad P ^a   Oosterom, Julia ^b   Timmers, Cornelis M ^b   Overkleeft, Herman S ^a   van der Marel, Gijsbert A ^a  

^a LEIDEN UNIVERSITY   (Netherlands)

^b NV ORGANON   (Netherlands)

Author keywords

Allosteric interaction; Antagonist; Bivalent ligand; Dimerization; G protein coupled receptor; Gonadotropin releasing hormone receptor; Imidazopyrimidinone

Indexed keywords

BENZENE; GONADORELIN RECEPTOR; GONADORELIN RECEPTOR ANTAGONIST; HORMONE RECEPTOR BLOCKING AGENT; LIGAND; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; BIOLOGICAL ACTIVITY; CONTROLLED STUDY; DIMERIZATION; DRUG DESIGN; DRUG SCREENING; DRUG SYNTHESIS; FEMALE; NONHUMAN;

AMINO ACIDS; ANIMALS; BENZENE; CELL SURVIVAL; CHO CELLS; CRICETINAE; CRICETULUS; DATABASES, PROTEIN; DIMERIZATION; HUMANS; IODIDES; LIGANDS; MOLECULAR STRUCTURE; PARGYLINE; RECEPTORS, LHRH; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 41649108197     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2008.01.054     Document Type: Article

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