Discovery of novel non-carboxylic acid 5-amino-4-cyanopyrazole derivatives as potent and highly selective LPA1R antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 18, 2014, Pages 4450-4454

  Sidduri, Achyutharao ^a   Budd, David C ^a   Fuentes, Maria E ^a   Lambros, Ted ^a   Ren, Yonglin ^a   Roongta, Vikram ^a   Schoenfeld, Ryan C ^a   Gillespie, Paul ^a   Stevenson, Christopher S ^a   Truitt, Theresa ^a   Qian, Yimin ^a  

^a HOFFMANN LA ROCHE INC   (United States)

Author keywords

Novel LPA1 antagonists

Indexed keywords

3 ALKYLAMINO 2 ARYL 5H IMIDAZO [1,2 B]PYRAZOL 7 CARBONITRILE; DIMETHYL SULFOXIDE; LYSOPHOSPHATIDIC ACID 1 RECEPTOR ANTAGONIST; PYRAZOLE DERIVATIVE; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG; 5-AMINO-4-CYANOPYRAZOLE; LYSOPHOSPHATIDIC ACID; LYSOPHOSPHATIDIC ACID RECEPTOR; LYSOPHOSPHOLIPID;

ARTICLE; BRDU ASSAY; CELL PROLIFERATION; DRUG DEGRADATION; DRUG DEVELOPMENT; DRUG HYDROLYSIS; DRUG ISOLATION; DRUG SCREENING; DRUG STRUCTURE; HUMAN; IC50; LIQUID CHROMATOGRAPHY; LUNG FIBROBLAST; MASS SPECTROMETRY; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; CYTOLOGY; DOSE RESPONSE; DRUG EFFECTS; FIBROBLAST; LUNG; METABOLISM; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

CELL PROLIFERATION; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; FIBROBLASTS; HUMANS; LUNG; LYSOPHOSPHOLIPIDS; MOLECULAR STRUCTURE; PYRAZOLES; RECEPTORS, LYSOPHOSPHATIDIC ACID; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84906967384     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.08.001     Document Type: Article

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