Synthesis and optimization of an original V-shaped collection of 4-7-disubstituted Pyrido[3,2-d]pyrimidines as CDK5 and DYRK1A inhibitors

European Journal of Medicinal Chemistry

Volumn 80, Issue , 2014, Pages 352-363

  Dehbi, Oussama ^a,b   Tikad, Abdellatif ^a,b   Bourg, Stephane ^a   Bonnet, Pascal ^a   Lozach, Olivier ^c   Meijer, Laurent ^c   Aadil, Mina ^b   Akssira, Mohammed ^b   Guillaumet, Gérald ^a   Routier, Sylvain ^a  

^a Université d'Orléans   (France)

^b HASSAN II UNIVERSITY   (Morocco)

^c Protein Phosphorylation and Human Disease Group   (France)

Author keywords

CDK5; DYRK1A; Molecular modelling; Pyridopyrimidine; SAR; Synthesis

Indexed keywords

4 (7 (4 HYDROXYPHENYL)PYRIDO[3,2 D]PYRIMIDIN 2 YL) THIOPHENE 2 CARBALDE HYDE; 4 (7 (4 HYDROXYPHENYL)PYRIDO[3,2 D]PYRIMIDIN 2 YL) THIOPHENE 3 CARBALDEHYDE; 4 (7 (5 (4 METHYLPIPERAZIN 1 YLMETHYLTHIOPHEN 3 YL)PYRIDO [3,2 D]PYRIMIDIN 2 YL)PHENOL; 4 (7 (5 (MORPHOLINOMETHYL)THIOPHEN 3 YL)PYRIDO[3,2 D] PYRIMIDIN 2 YL)PHENOL; 4 (7 (5 (PIPERIDIN 1 YLMETHYL)THIOPHEN 3 YL)PYRIDO[3,2 D] PYRIMIDIN 2 YL)PHENOL; 4 [7 (2 (METHYL)PYRIDINYLAMINO) PYRIDO[3,2 D]PYRIMIDIN 2 YL] PHENOL; 4 [7 (4 METHOXY PHENYLAMINO) PYRIDO[3,2 D]PYRIMIDIN 2 YL] PHENOL; 4 [7 (4 METHYL THIAZOL 2 YLAMINO) PYRIDO[3,2 D]PYRIMIDIN 2 YL] PHENOL; 4 [7 (5 (CYANO)PYRIDINYLAMINO] PYRIDO[3,2 D]PYRIMIDIN 2 YL] PHENOL; 4 [7 (5 METHYL THIOPHEN 3 YL) PYRIDO[3,2 D]PYRIMIDIN 2 YL] PHENOL; 4 [7 (BENZOTHIAZOL 2 YLAMINO) PYRIDO[3,2 D]PYRIMIDIN 2 YL] PHENOL; 4 [7 (ISOXAZOL 3 YLAMINO) PYRIDO[3,2 D]PYRIMIDIN 2 YL] PHENOL; 4 [7 (PYRIDIN 2 YLAMINO) PYRIDO[3,2 D]PYRIMIDIN 2 YL] PHENOL; 4 [7 (PYRIDIN 3 YLAMINO) PYRIDO[3,2 D]PYRIMIDIN 2 YL] PHENOL; 4 [7 (PYRIDIN 4 YLAMINO) PYRIDO[3,2 D]PYRIMIDIN 2 YL] PHENOL; 4 [7 (PYRIMIDIN 2 YLAMINO) PYRIDO[3,2 D]PYRIMIDIN 2 YL] PHENOL; 4 [7 (THIAZOL 2 YLAMINO) PYRIDO[3,2 D]PYRIMIDIN 2 YL] PHENOL; 7 (4 (4 HYDROXYPHENYL)PYRIDO[3,2 D]PYRIMIDIN 2 YL) THIOPHENE 3 CARBALDE HYDE; BORON DERIVATIVE; CYCLIN DEPENDENT KINASE 5; DUAL SPECIFICITY PHOSPHATASE; DUAL SPECIFICITY TYROSINE PHOSPHORYLATION REGULATED KINASE 1A; HETEROCYCLIC COMPOUND; N [2 (4 HYDROXYPHENYL) PYRIDO[3,2 D]PYRIMIDIN 7 YL] ISONICOTINAMIDE; N [2 (4 HYDROXYPHENYL) PYRIDO[3,2 D]PYRIMIDIN 7 YL] NICOTINAMIDE; OXAZOLE DERIVATIVE; PHOSPHOTRANSFERASE INHIBITOR; PROTEIN KINASE; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; DYRK KINASE; GLYCOGEN SYNTHASE KINASE 3; PROTEIN KINASE INHIBITOR; PROTEIN SERINE THREONINE KINASE; PROTEIN TYROSINE KINASE; PYRIMIDINE;

ARTICLE; BIOLOGICAL ACTIVITY; CONTROLLED STUDY; CROSS COUPLING REACTION; DRUG SCREENING; DRUG SYNTHESIS; ENZYME INHIBITION; HYDROGEN BOND; MOLECULAR DOCKING; STRUCTURE ACTIVITY RELATION; SUZUKI REACTION; ANTAGONISTS AND INHIBITORS; CHEMISTRY; ENZYME ACTIVE SITE; HUMAN; METABOLISM; SYNTHESIS;

CATALYTIC DOMAIN; CHEMISTRY TECHNIQUES, SYNTHETIC; CYCLIN-DEPENDENT KINASE 5; GLYCOGEN SYNTHASE KINASE 3; HUMANS; MOLECULAR DOCKING SIMULATION; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; PROTEIN-TYROSINE KINASES; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84899873885     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2014.04.055     Document Type: Article

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