Synthesis and biological evaluation of substituted benzoxazoles as inhibitors of mPGES-1: Use of a conformation-based hypothesis to facilitate compound design

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 4, 2013, Pages 1120-1126

  Walker, Daniel P ^a   Arhancet, Graciela B ^a   Lu, Hwang Fun ^a   Heasley, Steven E ^a   Metz, Sue ^a   Kablaoui, Natasha M ^a   Franco, Francisco M ^a   Hanau, Cathleen E ^a   Scholten, Jeffrey A ^a   Springer, John R ^a   Fobian, Yvette M ^a   Carter, Jeffrey S ^a   Xing, Li ^a   Yang, Shengtian ^a   Shaffer, Alexander F ^a   Jerome, Gina M ^a   Baratta, Michael T ^a   Moore, William M ^a   Vazquez, Michael L ^a  

^a PFIZER INC   (United States)

Author keywords

Acyl glucuronide; Benzoxazole; Conformational analysis; mPGES 1; Solubility

Indexed keywords

2 (3',4' DIMETHOXYBENZOYL) 6 METHYLPYRIDINE THIOSEMICARBAZONE DERIVATIVE; 2 (4' METHOXYBENZOYL) 6 METHYLPYRIDINE THIOSEMICARBAZONE DERIVATIVE; 2 BENZOYL 6 METHYLPYRIDINE THIOSEMICARBAZONE DERIVATIVE; ANTINEOPLASTIC AGENT; DEFEROXAMINE; IRON 59; IRON CHELATING AGENT; PHENYL GROUP; PYRIDINE; THIOSEMICARBAZONE DERIVATIVE; UNCLASSIFIED DRUG; BENZOXAZOLE DERIVATIVE; CYCLOHEXANE; MICROSOMAL PROSTAGLANDIN E2 SYNTHASE 1; PF 04693627; PROSTAGLANDIN SYNTHASE; PROSTAGLANDIN SYNTHASE INHIBITOR; ENZYME INHIBITOR; ISOMERASE; PROSTAGLANDIN E SYNTHASE;

ANTINEOPLASTIC ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; ARTICLE; CHELATION; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG DESIGN; DRUG EFFICACY; DRUG POTENCY; DRUG SYNTHESIS; ELECTRON TRANSPORT; GOLD STANDARD; HUMAN; HUMAN CELL; IC 50; IRON BINDING CAPACITY; LIPOPHILICITY; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; TUMOR CELL; ARTHRITIS; DRUG CONFORMATION; DRUG SCREENING; ENZYME ACTIVITY; HYPOTHESIS; IN VIVO STUDY; MICROSOME; NONHUMAN; RAT; CHEMICAL STRUCTURE; CHEMISTRY; CONFORMATION; DRUG ANTAGONISM; METABOLISM; SYNTHESIS;

BENZOXAZOLES; DRUG DESIGN; ENZYME INHIBITORS; HUMANS; INTRAMOLECULAR OXIDOREDUCTASES; MODELS, MOLECULAR; MOLECULAR CONFORMATION; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84875698221     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.11.107     Document Type: Article

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