Targeting the Warburg Effect in cancer; Relationships for 2-arylpyridazinones as inhibitors of the key glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3)

Bioorganic and Medicinal Chemistry

Volumn 22, Issue 3, 2014, Pages 1029-1039

  Brooke, Darby G ^a   Van Dam, Ellen M ^b   Watts, Colin K W ^b   Khoury, Amanda ^b   Dziadek, Marie A ^b   Brooks, Hilary ^b   Graham, Lisa Jane K ^b   Flanagan, Jack U ^a,c   Denny, William A ^a,c  

^a UNIVERSITY OF AUCKLAND   (New Zealand)

^b GARVAN INSTITUTE OF MEDICAL RESEARCH   (Australia)

^c UNIVERSITY OF AUCKLAND   (New Zealand)

Author keywords

Glycolysis; PFKFB3; Pyridazinone; Warburg Effect

Indexed keywords

2 (5 BROMO 6 OXO 1 PHENYL 1,6 DIHYDROPYRIDAZIN 4 YL) 1,2,3,4 TETRAHYDROISOQUINOLINE 5 CARBONITRILE; 2 [(5 BROMO 6 OXO 1 PHENYL 1,6 DIHYDROPYRIDAZIN 4 YL)AMINO]ACETAMIDE; 2 ARYLPYRIDAZINONE DERIVATIVE; 4 [4 (4 ACETYL 5 METHYL 1H 1,2,3 TRIAZOL 1 YL) 5 BROMO 6 OXOPYRIDAZIN 1(6H)YL]BENZONITRILE; 4 BROMO 2 PHENYL 5 (2 OXA 6 AZASPIRO[3.3]HEPTAN 6 YL)PYRIDAZIN 3(2H)ONE; 4 BROMO 2 PHENYL 5 [[(TETRAHYDROFURAN 2 YL)METHYL]AMINO]PYRIDAZIN 3(2H)ONE; 4 BROMO 5 MORPHOLINO 2 PHENYLPYRIDAZIN 3(2H)ONE; 5 (4 ACETYL 5 METHYL 1H 1,2,3 TRIAZOL 1 YL) 2 BENZYL 4 BROMOPYRIDAZIN 3(2H)ONE; 5 (4 ACETYL 5 METHYL 1H 1,2,3 TRIAZOL 1 YL) 2 BENZYLPYRIDAZIN 3(2H)ONE; 5 (4 ACETYL 5 METHYL 1H 1,2,3 TRIAZOL 1 YL) 4 BROMO 2 (3 PHENYLPROPYL)PYRIDAZIN 3(2H)ONE; 5 (4 ACETYL 5 METHYL 1H 1,2,3 TRIAZOL 1 YL) 4 BROMO 2 (4 CHLOROPHENYL)PYRIDAZIN 3(2H)ONE; 5 (4 ACETYL 5 METHYL 1H 1,2,3 TRIAZOL 1 YL) 4 BROMO 2 (4 IODOBENZYL)PYRIDAZIN 3(2H)ONE; 5 (4 ACETYL 5 METHYL 1H 1,2,3 TRIAZOL 1 YL) 4 BROMO 2 (PYRIMIDIN 5 YL)PYRIDAZIN 3(2H)ONE; 5 (4 ACETYL 5 METHYL 1H 1,2,3 TRIAZOL 1 YL) 4 BROMO 2 [4 (TRIFLUOROMETHOXY)PHENYL]PYRIDAZIN 3(2H)ONE; 5 (4 ACETYL 5 METHYL 1H 1,2,3 TRIAZOL 1 YL) 4 BROMO 2 [4 [[2 (DIMETHYLAMINO)ETHYL]AMINO]BENZYL]PYRIDAZIN 3(2H)ONE; 5 (4 ACETYL 5 METHYL 1H 1,2,3 TRIAZOL 1 YL) 4 BROMO 2 PHENETHYLPYRIDAZIN 3(2H)ONE; 5 (4 ACETYL 5 METHYL 1H 1,2,3 TRIAZOL 1 YL) 4 BROMO 2 PHENYLPYRIDAZIN 3(2H)ONE; 5 (4 ACETYL 5 METHYL 1H 1,2,3 TRIAZOL 1 YL) 4 CHLORO 2 PHENYLPYRIDAZIN 3(2H)ONE; 5 (4 ACETYL 5 METHYL 1H 1,2,3 TRIAZOL 1 YL) 4 ETHOXY 2 PHENYLPYRIDAZIN 3(2H)ONE; 5 (4 ACETYL 5 METHYL 1H 1,2,3 TRIAZOL 1 YL) 4 IODO 2 PHENYLPYRIDAZIN 3(2H)ONE; 5 (4 ACETYL 5 METHYL 1H 1,2,3 TRIAZOL 1 YL) 4 ISOPROPYL 2 PHENYLPYRIDAZIN 3(2H)ONE; 6 PHOSPHOFRUCTO 2 KINASE 2,6 BISPHOSPHATASE 3; ETHYL 1 [6 OXO 1 PHENYL 5 (2 OXA 6 AZASPIRO[3.3]HEPTAN 6 YL) 1,6 DIHYDROPYRIDAZIN 4 YL] 1H 1,2,3 TRIAZOLE 4 CARBOXYLATE; GLYCOLYTIC ENZYME; LACTIC ACID; PYRIDAZINONE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TARGETING; ENZYME INHIBITION; GLYCOLYSIS; HIGH THROUGHPUT SCREENING; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION;

(2,2,6,2-TETRAMETHYLPIPERIDIN-1-YL)OXY; 6-PHOSPHOFRUCTO-1-KINASE; 6-PHOSPHOFRUCTO-2-KINASE/2,6-BISPHOSPHATASE 3; BCA; BICINCHONINIC ACID ASSAY; ECAR; EXTRACELLULAR ACIDIFICATION RATE; F1,6-BP; F2,6-BP; F6P; FRUCTOSE-1,6-BISPHOSPHATE; FRUCTOSE-2,6-BISPHOSPHATE; FRUCTOSE-6-PHOSPHATE; GLYCOLYSIS; PFK-1; PFKFB3; PYRIDAZINONE; RADIOIMMUNOPRECIPITATION ASSAY; RIPA; TEMPO; WARBURG EFFECT;

ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; CHEMISTRY TECHNIQUES, SYNTHETIC; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; GLYCOLYSIS; HUMANS; MOLECULAR DOCKING SIMULATION; MOLECULAR STRUCTURE; PHOSPHOFRUCTOKINASE-2; PYRIDAZINES; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84892821916     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2013.12.041     Document Type: Article

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