Novel glucocorticoids containing a 6,5-bicyclic core fused to a pyrazole ring: Synthesis, in vitro profile, molecular modeling studies, and in vivo experiments

Bioorganic and Medicinal Chemistry Letters

Volumn 17, Issue 12, 2007, Pages 3354-3361

  Thompson, Christopher F ^a   Quraishi, Nazia ^a   Ali, Amjad ^a   Mosley, Ralph T ^a   Tata, James R ^a   Hammond, Milton L ^a   Balkovec, James M ^a   Einstein, Monica ^a   Ge, Lan ^a   Harris, Georgianna ^a   Kelly, Terri M ^a   Mazur, Paul ^a   Pandit, Shilpa ^a   Santoro, Joseph ^a   Sitlani, Ayesha ^a   Wang, Chuanlin ^a   Williamson, Joanne ^a   Miller, Douglas K ^a   Yamin, Ting ting D ^a   Thompson, Chris M ^a   O'Neill, Edward A ^a   Zaller, Dennis ^a   Forrest, Michael J ^a   Carballo Jane, Ester ^a   Luell, Silvi ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Dissociation; Glucocorticoid; Inflammation; Transactivation; Transrepression

Indexed keywords

DEXAMETHASONE; GLUCOCORTICOID; PREDNISOLONE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIINFLAMMATORY ACTIVITY; AREA UNDER THE CURVE; ARTICLE; DRUG BIOAVAILABILITY; DRUG CONFORMATION; DRUG HALF LIFE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; INFLAMMATION; MOLECULAR MODEL; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION;

ANIMALS; ANTINEOPLASTIC AGENTS; BICYCLO COMPOUNDS; CELL LINE, TUMOR; GLUCOCORTICOIDS; HUMANS; LIGANDS; MICE; MODELS, CHEMICAL; MODELS, MOLECULAR; PYRAZOLES; RECEPTORS, GLUCOCORTICOID; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 34249279834     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.03.103     Document Type: Article

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50. 50 = 3.3 nM (67% dex). 26 was not prepared in sufficient quantity to be tested in vivo.