Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors

Bioorganic and Medicinal Chemistry

Volumn 22, Issue 17, 2014, Pages 4998-5012

  Brasca, Maria Gabriella ^a   Nesi, Marcella ^a   Avanzi, Nilla ^a   Ballinari, Dario ^a   Bandiera, Tiziano ^a   Bertrand, Jay ^a   Bindi, Simona ^a   Canevari, Giulia ^a   Carenzi, Davide ^a   Casero, Daniele ^a   Ceriani, Lucio ^a   Ciomei, Marina ^a   Cirla, Alessandra ^a   Colombo, Maristella ^a   Cribioli, Sabrina ^a   Cristiani, Cinzia ^a   Della Vedova, Franco ^a   Fachin, Gabriele ^a   Fasolini, Marina ^a   Felder, Eduard R ^a   Galvani, Arturo ^a   Isacchi, Antonella ^a   Mirizzi, Danilo ^a   Motto, Ilaria ^a   Panzeri, Achille ^a   Pesenti, Enrico ^a   Vianello, Paola ^a   Gnocchi, Paola ^a   Donati, Daniele ^a   more..

^a NERVIANO MEDICAL SCIENCES   (Italy)

Author keywords

Anti cancer agents; JAK2; Myeloproliferative disorders; Protein kinase inhibitor; Tumour cell proliferation inhibition

Indexed keywords

3 PYRROLECARBOXAMIDE DERIVATIVE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (2 CHLORO 5 METHYLPHENYL) 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (2 CHLOROPHENYL) 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (2 METHYLPHENYL) 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (2,5 DICHLOROPHENYL) 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (3 CHLOROPHENYL) 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (5 CHLORO 2 ETHYLPHENYL) 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (5 CHLORO 2 METHOXYPHENYL) 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (5 CHLORO 2 METHYLPHENYL) 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (5 CHLORO 2 METHYLPHENYL) N (2 FLUOROETHYL) 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (5 CHLORO 2 METHYLPHENYL) N (2 HYDROXYETHYL) 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (5 CHLORO 2 METHYLPHENYL) N (2 METHOXYETHYL) 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (5 CHLORO 2 METHYLPHENYL) N (2 METHYLPROPYL) 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (5 CHLORO 2 METHYLPHENYL) N ETHYL 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (5 CHLORO 2 METHYLPHENYL) N METHYL 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (5 CHLORO 2 METHYLPHENYL) N PHENYL 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (5 CHLORO 2 METHYLPHENYL) N [2 (METHYLAMINO)ETHYL] 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 (5 CHLORO 2 METHYLPHENYL) N,N DIMETHYL 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 PHENYL 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 [2 CHLORO 5 (TRIFLUOROMETHYL)PHENYL] 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 [2 ETHYL 5 (TRIFLUOROMETHYL)PHENYL] 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 [2 METHYL 5 (TRIFLUOROMETHOXY)PHENYL] 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 [2 METHYL 5 (TRIFLUOROMETHYL)PHENYL] 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 [2,5 BIS (TRIFLUOROMETHYL)PHENYL] 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 [5 CHLORO 2 (PROPAN 2 YL)PHENYL] 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) 2 [5 CHLORO 2 (TRIFLUOROMETHYL)PHENYL] 1H PYRROLE 3 CARBOXAMIDE; 5 (2 AMINOPYRIMIDIN 4 YL) N BENZYL 2 (2 CHLORO 5 METHYLPHENYL) 1H PYRROLE 3 CARBOXAMIDE; BIOLOGICAL MARKER; JANUS KINASE 2 INHIBITOR; UNCLASSIFIED DRUG; UNINDEXED DRUG; 5-(2-AMINOPYRIMIDIN-4-YL)-2-(2-CHLORO-5-(TRIFLUOROMETHYL)PHENYL)-1H-PYRROLE-3-CARBOXAMIDE; ANTINEOPLASTIC AGENT; JANUS KINASE 2; PROTEIN KINASE INHIBITOR; PYRIMIDINE DERIVATIVE; PYRROLE DERIVATIVE;

ACUTE MEGAKARYOCYTIC LEUKEMIA; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CANCER INHIBITION; CELL PROLIFERATION; CONTROLLED STUDY; DRUG CLEARANCE; DRUG DESIGN; DRUG EFFICACY; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG MECHANISM; DRUG STRUCTURE; DRUG SYNTHESIS; FEMALE; HUMAN; HUMAN CELL; IN VIVO STUDY; LEUKEMIA CELL LINE; MALE; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; SET 2 CELL LINE; STRUCTURE ACTIVITY RELATION; TUMOR XENOGRAFT; VOLUME OF DISTRIBUTION; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG EFFECTS; DRUG SCREENING; ENZYME SPECIFICITY; METABOLISM; NEOPLASMS, EXPERIMENTAL; PATHOLOGY; SCID MOUSE; SYNTHESIS; TUMOR CELL LINE; X RAY CRYSTALLOGRAPHY;

ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; CELL PROLIFERATION; CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG SCREENING ASSAYS, ANTITUMOR; HUMANS; JANUS KINASE 2; MICE; MICE, SCID; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NEOPLASMS, EXPERIMENTAL; PROTEIN KINASE INHIBITORS; PYRIMIDINES; PYRROLES; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY;

EID: 84921997858     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2014.06.025     Document Type: Article

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