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Literature summary for 3.1.6.2 extracted from

  • Malini, B.; Purohit, A.; Ganeshapillai, D.; Woo, L.W.L.; Potter, B.V.L.; Reed, M.J.
    Inhibition of steroid sulphatase activity by tricyclic coumarin sulphamates (2000), J. Steroid Biochem. Mol. Biol., 75, 253-258.
    View publication on PubMed
Search for more literature for 3.1.6.2

Application

Application Comment Organism
pharmacology inhibition of STS is an important target for the development of new drugs for oncology and immunology Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
4-methylcoumarin-7-O-sulfamate
-
 Rattus norvegicus
4-oxo-2,3-dihydro-1H-cyclopenta-[c][1]benzopyran-7-O-sulfamate 665 COUMATE, placental IC50: 200 nM Rattus norvegicus
6-oxo-7,8,9,10,11,12,13,14,15,16-decahydro-cyclododeca-[c][1]benzopyran-3-O-sulfamate 6612 COUMATE, placental IC50: 60 nM Rattus norvegicus
6-oxo-7,8,9,10,11,12,13,14-octahydro-cyclodeca-[c][1]benzopyran-3-O-sulfamate 6610 COUMATE, placental IC50: 1 nM Rattus norvegicus
6-oxo-7,8,9,10,11,12-hexahydro-cycloocta-[c][1]benzopyran-3-O-sulfamate 668 COUMATE, placental IC50: 30 nM Rattus norvegicus
6-oxo-7,8,9,10-tetrahydro-dibenzo[b,d]pyran-3-O-sulfamate 666 COUMATE, placental IC50: 70 nM Rattus norvegicus
6-oxo-8,9,10,11,12,13,14,15,16,17,18,19-dodecahydro-7H-cyclopentadeca-[c][1]benzopyran-3-O-sulfamate 6615 COUMATE, placental IC50: 370 nM, most potent tricyclic coumarin sulfamate inhibitor tested in vivo Rattus norvegicus
6-oxo-8,9,10,11,12,13,14,15,16,17-decahydro-7H-cyclotrideca-[c][1]benzopyran-3-O-sulfamate 6613 COUMATE, placental IC50: 75 nM Rattus norvegicus
6-oxo-8,9,10,11,12,13,14,15-octahydro-7H-cycloundeca-[c][1]benzopyran-3-O-sulfamate 6611 COUMATE, placental IC50: 13 nM Rattus norvegicus
6-oxo-8,9,10,11,12,13-hexahydro-7H-cyclonona-[c][1]benzopyran-3-O-sulfamate 669 COUMATE, placental IC50: 2.4 nM Rattus norvegicus
6-oxo-8,9,10,11-tetrahydro-7H-cyclohepta-[c][1]benzopyran-3-O-sulfamate 667 COUMATE, placental IC50: 8 nM Rattus norvegicus
tricyclic coumarin sulfamate in vitro and in vivo inhibition studies with E1-STS from different tissues, structure-activity relationship of a number of tricyclic coumarin sulfamates, the size of the third ring has a marked effect on inhibitor potency Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome placental Rattus norvegicus
-
-

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
 female Wistar rats
-

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
 Rattus norvegicus
-
liver
-
 Rattus norvegicus
-
placenta
-
 Rattus norvegicus
-
white blood cell
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
estrone sulfate + H2O
-
 Rattus norvegicus estrone + sulfate
-
 ?

Synonyms

Synonyms Comment Organism
E1-STS
-
 Rattus norvegicus
oestrone sulfatase
-
 Rattus norvegicus
STS
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000001
-
 6610 COUMATE, placental IC50: 1 nM Rattus norvegicus 6-oxo-7,8,9,10,11,12,13,14-octahydro-cyclodeca-[c][1]benzopyran-3-O-sulfamate
0.0000024
-
 669 COUMATE, placental IC50: 2.4 nM Rattus norvegicus 6-oxo-8,9,10,11,12,13-hexahydro-7H-cyclonona-[c][1]benzopyran-3-O-sulfamate
0.000008
-
 667 COUMATE, placental IC50: 8 nM Rattus norvegicus 6-oxo-8,9,10,11-tetrahydro-7H-cyclohepta-[c][1]benzopyran-3-O-sulfamate
0.000013
-
 6611 COUMATE, placental IC50: 13 nM Rattus norvegicus 6-oxo-8,9,10,11,12,13,14,15-octahydro-7H-cycloundeca-[c][1]benzopyran-3-O-sulfamate
0.00003
-
 668 COUMATE, placental IC50: 30 nM Rattus norvegicus 6-oxo-7,8,9,10,11,12-hexahydro-cycloocta-[c][1]benzopyran-3-O-sulfamate
0.00006
-
 6612 COUMATE, placental IC50: 60 nM Rattus norvegicus 6-oxo-7,8,9,10,11,12,13,14,15,16-decahydro-cyclododeca-[c][1]benzopyran-3-O-sulfamate
0.00007
-
 666 COUMATE, placental IC50: 70 nM Rattus norvegicus 6-oxo-7,8,9,10-tetrahydro-dibenzo[b,d]pyran-3-O-sulfamate
0.000075
-
 6613 COUMATE, placental IC50: 75 nM Rattus norvegicus 6-oxo-8,9,10,11,12,13,14,15,16,17-decahydro-7H-cyclotrideca-[c][1]benzopyran-3-O-sulfamate
0.0002
-
 665 COUMATE, placental IC50: 200 nM Rattus norvegicus 4-oxo-2,3-dihydro-1H-cyclopenta-[c][1]benzopyran-7-O-sulfamate
0.00037
-
 6615 COUMATE, placental IC50: 370 nM, most potent tricyclic coumarin sulfamate inhibitor tested in vivo Rattus norvegicus 6-oxo-8,9,10,11,12,13,14,15,16,17,18,19-dodecahydro-7H-cyclopentadeca-[c][1]benzopyran-3-O-sulfamate