Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: Improvements in physical properties enhance cellular activity and pharmacokinetics

Bioorganic and Medicinal Chemistry Letters

Volumn 12, Issue 24, 2002, Pages 3537-3541

  Fraley, Mark E ^a   Rubino, Robert S ^a   Hoffman, William F ^a   Hambaugh, Scott R ^a   Arrington, Kenneth L ^a   Hungate, Randall W ^a   Bilodeau, Mark T ^a   Tebben, Andrew J ^a   Rutledge, Ruth Z ^a   Kendall, Richard L ^a   McFall, Rosemary C ^a   Huckle, William R ^a   Coll, Kathleen E ^a   Thomas, Kenneth A ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

FIBROBLAST GROWTH FACTOR RECEPTOR 1; FIBROBLAST GROWTH FACTOR RECEPTOR 2; PLATELET DERIVED GROWTH FACTOR BETA RECEPTOR; PROTEIN TYROSINE KINASE INHIBITOR; PYRIMIDINE DERIVATIVE; VASCULOTROPIN RECEPTOR 2; ANGIOGENESIS INHIBITOR; ENZYME INHIBITOR;

ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TOLERABILITY; ENZYME INHIBITION; IC 50; MITOGENESIS; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; ANIMAL; CELL DIVISION; CELL LINE; DRUG ANTAGONISM; DRUG EFFECT; HUMAN; METABOLIC CLEARANCE RATE; PHARMACOKINETICS; SOLUBILITY; SYNTHESIS; VASCULAR ENDOTHELIUM;

ANGIOGENESIS INHIBITORS; ANIMALS; CELL DIVISION; CELL LINE; ENDOTHELIUM, VASCULAR; ENZYME INHIBITORS; HUMANS; INHIBITORY CONCENTRATION 50; METABOLIC CLEARANCE RATE; PHARMACOKINETICS; PYRIMIDINES; RATS; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP; VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR-2;

EID: 17744412817     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(02)00827-2     Document Type: Article

References (31)

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