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Literature summary for 2.7.1.40 extracted from

  • Walsh, M.J.; Brimacombe, K.R.; Veith, H.; Bougie, J.M.; Daniel, T.; Leister, W.; Cantley, L.C.; Israelsen, W.J.; Vander Heiden, M.G.; Shen, M.; Auld, D.S.; Thomas, C.J.; Boxer, M.B.
    2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase (2011), Bioorg. Med. Chem. Lett., 21, 6322-6327.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.1.40

Activating Compound

Activating Compound Comment Organism Structure
1-acetyl-N-(3,4-dimethylphenyl)-1,2,3,4-tetrahydroquinoline-8-sulfonamide
-
 Homo sapiens
1-acetyl-N-(3,4-dimethylphenyl)-2,3-dihydro-1H-indole-5-sulfonamide
-
 Homo sapiens
2-oxo-N-(pyridin-3-yl)-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
2-oxo-N-(pyridin-4-yl)-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
2-oxo-N-(quinolin-6-yl)-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
2-oxo-N-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
3-chloro-N-(3,4-dimethylphenyl)benzenesulfonamide
-
 Homo sapiens
3-fluorophenyl (3,4-dimethylphenyl)sulfamate
-
 Homo sapiens
3-[(3,4-dimethylphenyl)sulfamoyl]benzoic acid
-
 Homo sapiens
3-{[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-1,4-diazepan-1-yl]sulfonyl}aniline i.e. NCGC00185916 Homo sapiens
4-fluorophenyl (3,4-dimethylphenyl)sulfamate
-
 Homo sapiens
5-amino-N-(3,4-dimethylphenyl)-1-methyl-1H-indole-7-sulfonamide
-
 Homo sapiens
6-(3-methoxybenzyl)-4-methyl-2-(methylsulfinyl)-4,6-dihydro-5H-thieno[2',3':4,5]pyrrolo[2,3-d]pyridazin-5-one i.e. NCGC00186527 Homo sapiens
6-chloro-N-(3,4-dimethylphenyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide
-
 Homo sapiens
7-(chloroamino)-N-(3,4-dimethylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
7-(diethylamino)-N-(3,4-dimethylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
7-(dimethylamino)-N-(3,4-dimethylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
7-(fluoroamino)-N-(3-fluoro-4-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
7-bromo-N-(3,4-dimethylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
7-bromo-N-(4-chloro-3-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
7-chloro-N-(4-chloro-3-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
7-[3-(dimethylamino)pyrrolidin-1-yl]-N-(3,4-dimethylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
additional information 2-oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase, synthesis, structure-activity relationships, selectivity, and notable physiochemical properties are, overview Homo sapiens
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(2,3-dihydro-1H-inden-5-yl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(2-fluorophenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(2-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3,4-dichlorophenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-1-methyl-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-2,2-dimethyl-3,4-dihydro-2H-chromene-6-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-7-sulfonamide i.e. NCGC00185939 Homo sapiens
N-(3,4-dimethylphenyl)-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine-7-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-2-oxo-2,3-dihydro-1H-benzimidazole-4-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-2-oxo-2,3-dihydro-1H-indole-4-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-2-oxo-7-(piperidin-1-yl)-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-2-oxo-7-(propan-2-ylamino)-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-2-oxo-7-(pyrrolidin-1-yl)-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazole-5-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-6-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-3-oxo-6-phenyl-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-3-oxo-6-[(E)-2-phenylethenyl]-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-4-(2-oxopyrrolidin-1-yl)benzenesulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-4-fluorobenzenesulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-4-methoxybenzenesulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-4-methyl-3,4-dihydro-2H-1,4-benzoxazine-6-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-6-fluoro-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-6-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-7-(methylamino)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-7-[(1-hydroxypropan-2-yl)amino]-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-7-[(2-hydroxyethyl)amino]-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-7-[(2-hydroxypropan-2-yl)amino]-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-7-{[(2R)-1-hydroxypropan-2-yl]amino}-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)-7-{[(2S)-1-hydroxypropan-2-yl]amino}-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3,4-dimethylphenyl)naphthalene-2-sulfonamide
-
 Homo sapiens
N-(3-chloro-4-fluorophenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3-chloro-4-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3-chloro-4-methylphenyl)-7-(fluoroamino)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3-chlorophenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3-fluoro-4-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3-fluoro-4-methylphenyl)-7-{[(2S)-1-hydroxypropan-2-yl]amino}-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3-methoxyphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(3-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(4-chloro-3-fluorophenyl)-7-(fluoroamino)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(4-chloro-3-fluorophenyl)-7-{[(2S)-1-hydroxypropan-2-yl]amino}-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(4-chloro-3-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(4-chloro-3-methylphenyl)-7-(fluoroamino)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(4-chloro-3-methylphenyl)-7-{[(2S)-1-hydroxypropan-2-yl]amino}-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(4-chlorophenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(4-fluoro-3-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(4-methoxyphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(4-methylphenyl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(biphenyl-3-yl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-(naphthalen-2-yl)-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
 Homo sapiens
N-{3-[(3,4-dimethylphenyl)sulfamoyl]phenyl}acetamide
-
 Homo sapiens
N-{4-[(3,4-dimethylphenyl)sulfamoyl]phenyl}acetamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
additional information while the M1 isoform is a highly active enzyme, the alternatively spliced M2 variant is considerably less active and expressed in tumors Homo sapiens
-

Synonyms

Synonyms Comment Organism
PKM2
-
 Homo sapiens

General Information

General Information Comment Organism
physiological function the expression of the M2 isozyme of pyruvate kinase plays an important role in the anabolic metabolism of cancer cells Homo sapiens