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Literature summary for 3.1.6.2 extracted from

  • Woo, L.W.; Jackson, T.; Putey, A.; Cozier, G.; Leonard, P.; Acharya, K.R.; Chander, S.K.; Purohit, A.; Reed, M.J.; Potter, B.V.
    Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template (2010), J. Med. Chem., 53, 2155-2170.
    View publication on PubMed
Search for more literature for 3.1.6.2

Inhibitors

Inhibitors Comment Organism Structure
(12aS)-N,N-dihydroxy-12a-methyl-1,3-dioxo-2-propyl-1,2,3,4,4a,4b,5,6,10b,11,12,12a-dodecahydronaphtho[2,1-f]isoquinoline-8-sulfinamide
-
 Homo sapiens
2',4'-dicyano-N,N-dihydroxybiphenyl-4-sulfinamide
-
 Homo sapiens
2-bromo-4-[(R)-(4-cyanophenyl)(1H-1,2,4-triazol-1-yl)methyl]-N,N-dihydroxybenzenesulfinamide
-
 Homo sapiens
2-[3-[[(4-[[(aminooxy)sulfinyl]oxy]phenyl)sulfanyl]methyl]-5-(1H-1,2,4-triazol-1-ylmethyl)phenyl]-2-methylpropanenitrile
-
 Homo sapiens
3'-((1H-1,2,4-triazol-1-yl)methyl)-3-chloro-4'-cyanobiphenyl-4-yl sulfamate
-
 Homo sapiens
3'-((1H-1,2,4-triazol-1-yl)methyl)-3-chloro-5'-(2-cyanopropan-2-yl)biphenyl-4-yl sulfamate 68.2% inhibition at 0.01 mM Homo sapiens
3'-((1H-1,2,4-triazol-1-yl)methyl)-3-chloro-5'-cyanobiphenyl-4-yl sulfamate
-
 Homo sapiens
3'-((1H-1,2,4-triazol-1-yl)methyl)-3-chlorobiphenyl-4-yl sulfamate
-
 Homo sapiens
3'-((1H-1,2,4-triazol-1-yl)methyl)-4'-cyanobiphenyl-4-yl sulfamate
-
 Homo sapiens
3'-((1H-1,2,4-triazol-1-yl)methyl)biphenyl-4-yl sulfamate
-
 Homo sapiens
3'-chloro-5-(1H-1,2,4-triazol-1-ylmethyl)biphenyl-2-carbonitrile
-
 Homo sapiens
4'-((1H-1,2,4-triazol-1-yl)methyl)-2'-cyanobiphenyl-4-yl sulfamate
-
 Homo sapiens
4'-((1H-1,2,4-triazol-1-yl)methyl)-3-chloro-2'-cyanobiphenyl-4-yl sulfamate
-
 Homo sapiens
5'-((1H-1,2,4-triazol-1-yl)methyl)-2'-cyanobiphenyl-4-yl sulfamate
-
 Homo sapiens
5'-((1H-1,2,4-triazol-1-yl)methyl)-3-chloro-2'-cyanobiphenyl-4-yl sulfamate
-
 Homo sapiens
5-((1H-1,2,4-triazol-1-yl)methyl)-3'-chloro-4'-hydroxybiphenyl-2-carbonitrile
-
 Homo sapiens
5-((1H-1,2,4-triazol-1-yl)methyl)-4'-hydroxybiphenyl-2-carbonitrile
-
 Homo sapiens
anastrozole
-
 Homo sapiens
additional information not inhibited by letrozole, 5'-((1H-1,2,4-triazol-1-yl)methyl)-2'-cyanobiphenyl-4-yl dimethylsulfamate, 5'-((1H-1,2,4-triazol-1-yl)methyl)-3-chloro-2'-cyanobiphenyl-4-yl dimethylsulfamate, 5'-((1H-1,2,4-triazol-1-yl)methyl)-4-chloro-2'-cyanobiphenyl-3-yl sulfamate, 3'-((1H-1,2,4-triazol-1-yl)methyl)-4'-cyanobiphenyl-3-yl sulfamate, 3'-((1H-1,2,4-triazol-1-yl)methyl)-5'-cyanobiphenyl-4-yl sulfamate, 2'-((1H-1,2,4-triazol-1-yl)methyl)-3-chloro-5'-cyanobiphenyl-4-yl sulfamate, and 3'-((1H-1,2,4-triazol-1-yl)methyl)-5'-(2-cyanopropan-2-yl)biphenyl-4-yl sulfamate Homo sapiens
N,N-dihydroxy-6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromene-3-sulfinamide
-
 Homo sapiens
N,N-dimethoxy-6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromene-3-sulfinamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
JEG-3 cell
-
 Homo sapiens
-
liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
estrone sulfate + H2O
-
 Homo sapiens estrone + sulfate
-
 ?

Synonyms

Synonyms Comment Organism
steroid sulfatase
-
 Homo sapiens
STS
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000015
-
-
 Homo sapiens N,N-dihydroxy-6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromene-3-sulfinamide
0.0000055
-
-
 Homo sapiens 5'-((1H-1,2,4-triazol-1-yl)methyl)-3-chloro-2'-cyanobiphenyl-4-yl sulfamate
0.0000163
-
-
 Homo sapiens 2',4'-dicyano-N,N-dihydroxybiphenyl-4-sulfinamide
0.0000286
-
-
 Homo sapiens 4'-((1H-1,2,4-triazol-1-yl)methyl)-2'-cyanobiphenyl-4-yl sulfamate
0.0000326
-
-
 Homo sapiens 3'-((1H-1,2,4-triazol-1-yl)methyl)-3-chloro-4'-cyanobiphenyl-4-yl sulfamate
0.000035
-
-
 Homo sapiens 5'-((1H-1,2,4-triazol-1-yl)methyl)-2'-cyanobiphenyl-4-yl sulfamate
0.00005
-
-
 Homo sapiens 4'-((1H-1,2,4-triazol-1-yl)methyl)-3-chloro-2'-cyanobiphenyl-4-yl sulfamate
0.00014
-
-
 Homo sapiens 3'-((1H-1,2,4-triazol-1-yl)methyl)-4'-cyanobiphenyl-4-yl sulfamate
0.00016
-
-
 Homo sapiens 3'-((1H-1,2,4-triazol-1-yl)methyl)-3-chlorobiphenyl-4-yl sulfamate
0.0055
-
-
 Homo sapiens 3'-((1H-1,2,4-triazol-1-yl)methyl)biphenyl-4-yl sulfamate
0.006333
-
-
 Homo sapiens 3'-((1H-1,2,4-triazol-1-yl)methyl)-3-chloro-5'-cyanobiphenyl-4-yl sulfamate