Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 15, 2011, Pages 4507-4511

  Caldarelli, Marina ^a   Angiolini, Mauro ^a   Disingrini, Teresa ^a   Donati, Daniele ^a   Guanci, Marco ^a   Nuvoloni, Stefano ^a   Posteri, Helena ^a   Quartieri, Francesca ^a   Silvagni, Marco ^a   Colombo, Riccardo ^a  

^a NERVIANO MEDICAL SCIENCES   (Italy)

Author keywords

Anticancer; Kinase selectivity; MPS1; SAR; TTK

Indexed keywords

ANTINEOPLASTIC AGENT; ENZYME INHIBITOR; MONOPOLAR SPINDLE 1 KINASE; PHOSPHOPROTEIN; PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE DERIVATIVE; PYRAZOLONE DERIVATIVE; QUINAZOLINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER INHIBITION; CELL MEMBRANE PERMEABILITY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG POTENCY; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IN VIVO STUDY; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; AMIDES; ANIMALS; CELL CYCLE PROTEINS; MICE; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; QUINAZOLINES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79960371035     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.05.122     Document Type: Article

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