Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl] amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor

Journal of Medicinal Chemistry

Volumn 52, Issue 16, 2009, Pages 5152-5163

  Brasca, Maria Gabriella ^a   Amboldi, Nadia ^a   Ballinari, Dario ^a   Cameron, Alexander ^a,b   Casale, Elena ^a   Cervi, Giovanni ^a   Colombo, Maristella ^a   Colotta, Francesco ^a   Croci, Valter ^a   D'Alessio, Roberto ^a   Fiorentini, Francesco ^a,c   Isacchi, Antonella ^a   Mercurio, Ciro ^a,d   Moretti, Walter ^a   Panzeri, Achille ^a   Pastori, Wilma ^a   Pevarello, Paolo ^a,e   Quartieri, Francesca ^a   Roletto, Fulvia ^a   Traquandi, Gabriella ^a   Vianello, Paola ^a   Vulpetti, Anna ^a,f   Ciomei, Marina ^a   more..

^a NERVIANO MEDICAL SCIENCES   (Italy)

^b DIAMOND LIGHT SOURCE LTD   (United Kingdom)

^c Accelera Srl   (Italy)

^d Genextra Group   (Italy)

^e Newron Pharmaceuticals   (Italy)

^f NOVARTIS PHARMA AG   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

1 METHYL 8 (PHENYLAMINO) 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; 1 METHYL 8 [(4 MORPHOLIN 4 YLPHENYL)AMINO] 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; 1 METHYL 8 [[3 (4 METHYLPIPERAZIN 1 YL)PHENYL]AMINO] 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; 1 METHYL 8 [[4 (4 METHYLPIPERAZIN 1 YL)PHENYL]AMINO] 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; 1 METHYL N PHENYL 8 (PHENYLAMINO) 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; 1,4,4 TRIMETHYL 8 [[4 (4 METHYLPIPERAZIN 1 YL)PHENYL]AMINO] 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; 1,4,4 TRIMETHYL 8 PHENYLAMINO 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; 8 [[3 (DIMETHYLAMINO)PHENYL]AMINO] N,1,4,4 TETRAMETHYL 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; 8 [[4 (DIMETHYLAMINO)PHENYL]AMINO] N,1,4,4 TETRAMETHYL 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; 8 [[4 [(DIMETHYLAMINO)METHYL]PHENYL]AMINO] N,1,4,4 TETRAMETHYL 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; CYCLIN DEPENDENT KINASE INHIBITOR; N (2 HYDROXYETHYL) 1 METHYL 8 (PHENYLAMINO) 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; N BENZYL 1 METHYL 8 (PHENYLAMINO) 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; N CYCLOPENTYL 1 METHYL 8 (PHENYLAMINO) 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; N CYCLOPROPYL 1 METHYL 8 (PHENYLAMINO) 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; N,1 DIMETHYL 8 (PHENYLAMINO) 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; N,1 DIMETHYL 8 [[4 (4 METHYLPIPERAZIN 1 YL)PHENYL]AMINO] 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; N,1,4,4 TETRAMETHYL 8 [(3 MORPHOLIN 4 YLPHENYL)AMINO] 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; N,1,4,4 TETRAMETHYL 8 [(4 MORPHOLIN 4 YLPHENYL)AMINO] 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; N,1,4,4 TETRAMETHYL 8 [[3 (4 METHYLPIPERAZIN 1 YL)PHENYL]AMINO] 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; N,1,4,4 TETRAMETHYL 8 [[3 (MORPHOLIN 4 YLMETHYL)PHENYL]AMINO] 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; N,1,4,4 TETRAMETHYL 8 [[3 [(1 METHYLPIPERIDIN 4 YL)OXY]PHENYL]AMINO] 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; N,1,4,4 TETRAMETHYL 8 [[3 [(4 METHYLPIPERAZIN 1 YL)METHYL]PHENYL]AMINO] 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; N,1,4,4 TETRAMETHYL 8 [[4 (4 METHYLPIPERAZIN 1 YL)PHENYL]AMINO] 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; N,1,4,4 TETRAMETHYL 8 [[4 (MORPHOLIN 4 YLMETHYL)PHENYL]AMINO] 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; N,1,4,4 TETRAMETHYL 8 [[4 [(1 METHYLPIPERIDIN 4 YL)OXY]PHENYL]AMINO] 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; N,1,4,4 TETRAMETHYL 8 [[4 [(4 METHYLPIPERAZIN 1 YL)METHYL]PHENYL]AMINO] 4,5 DIHYDRO 1H PYRAZOLO[4,3 H]QUINAZOLINE 3 CARBOXAMIDE; PHA 848125; PROTEIN SERINE THREONINE KINASE; PROTEIN TYROSINE KINASE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CANCER CELL CULTURE; CANCER MODEL; CONTROLLED STUDY; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; DRUG TOLERABILITY; ENZYME ASSAY; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; MALE; MAXIMUM PLASMA CONCENTRATION; MITOSIS INHIBITION; MOUSE; NONHUMAN; PHYSICAL CHEMISTRY; STRUCTURE ANALYSIS; TUMOR XENOGRAFT;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; CELL PROLIFERATION; CRYSTALLOGRAPHY, X-RAY; CYCLIN-DEPENDENT KINASES; DRUG SCREENING ASSAYS, ANTITUMOR; HUMANS; MALE; MICE; MICE, NUDE; MODELS, MOLECULAR; NEOPLASM TRANSPLANTATION; PYRAZOLES; QUINAZOLINES; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSPLANTATION, HETEROLOGOUS;

EID: 69049103115     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm9006559     Document Type: Article

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