Page last updated: 2024-11-10

irosustat

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Description

irosustat: Antineoplastic Agents, Hormonal; a tricyclic sulfamate ester; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5287541
CHEMBL ID286738
SCHEMBL ID1275983
MeSH IDM0510718

Synonyms (51)

Synonym
6-oxo-8,9,10,11-tetrahydro-7h-cyclohepta[c][1]benzopyran-3-o-sulfamate
irosustat
1TTM
DB02292
chembl286738 ,
{9-oxo-8-oxatricyclo[8.5.0.0^{2,7}]pentadeca-1(10),2(7),3,5-tetraen-5-yl} sulfamate
stx64
bdbm13058
667-coumate
6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate
bn83495
667coumate
stx-64
bn-83495
stx 64
bn 83495
stx64 compound
6-oxo-8,9,10,11-tetrahydro-7h-cyclohepta-(c)(1)benzopyran-3-o-sulfamate
667 coumate
(6-oxo-8,9,10,11-tetrahydro-7h-cyclohepta[c]chromen-3-yl) sulfamate
D09915
irosustat (usan/inn)
288628-05-7
sulfamic acid, 6,7,8,9,10,11-hexahydro-6-oxobenzo(b)cyclohepta(d)pyran-3-yl ester
irosustat [usan:inn]
unii-366037o6o7
366037o6o7 ,
irosustat [inn]
irosustat [who-dd]
irosustat [usan]
6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c][1]benzopyran-3-yl sulfamate
S6558
SCHEMBL1275983
DTXSID50183059
stx64, >=98% (hplc)
J-017303
IROSUSTATSTX64 ,
CS-0003463
HY-14586
AKOS032954035
Q27093313
BCP29882
SB17271
6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate.
stx64;bn83495;667-coumate
sulfamic acid, 6,7,8,9,10,11-hexahydro-6-oxobenzo[b]cyclohepta[d]pyran-3-yl ester
AT25524
BS-52172
irosustat (stx-64)
irosustat (stx64, bn83495)
6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-ylsulfamate

Research Excerpts

Overview

Irosustat is a first-generation, irreversible, steroid sulfatase inhibitor currently in development for hormone-dependent cancer therapy.

ExcerptReferenceRelevance
"Irosustat is a novel steroid sulfatase inhibitor for hormone-dependent cancer therapy. "( In vitro metabolism of irosustat, a novel steroid sulfatase inhibitor: interspecies comparison, metabolite identification, and metabolic enzyme identification.
Celma, C; Obach, R; Peraire, C; Solà, J; Ventura, V, 2011
)
2.12
"Irosustat is a first-generation, irreversible, steroid sulfatase inhibitor currently in development for hormone-dependent cancer therapy. "( In vitro evaluation of the interaction potential of irosustat with drug-metabolizing enzymes.
Brée, F; Obach, R; Peraire, C; Solà, J; Ventura, V, 2012
)
2.07

Pharmacokinetics

The objective of this work was to develop a population model characterizing simultaneously the pharmacokinetic profiles of irosustat in plasma and whole blood.

ExcerptReferenceRelevance
" The objective of this work was to develop a population model characterizing simultaneously the pharmacokinetic profiles of irosustat in plasma and whole blood."( Population pharmacokinetic modelling of irosustat in postmenopausal women with oestrogen-receptor positive breast cancer incorporating non-linear red blood cell uptake.
Cendrós Carreras, JM; Chetaille, E; Obach, R; Parra-Guillen, ZP; Peraire, C; Prunynosa, J; Trocóniz, IF, 2015
)
0.89

Bioavailability

ExcerptReferenceRelevance
" Relative bioavailability was decreased as the administered dose was augmented."( Population pharmacokinetic modelling of irosustat in postmenopausal women with oestrogen-receptor positive breast cancer incorporating non-linear red blood cell uptake.
Cendrós Carreras, JM; Chetaille, E; Obach, R; Parra-Guillen, ZP; Peraire, C; Prunynosa, J; Trocóniz, IF, 2015
)
0.68

Dosage Studied

ExcerptRelevanceReference
" STX64 was administered orally (nine patients at 5 mg and five patients at 20 mg) as an initial dose followed 1 week later by 3 x 2 weekly cycles, with each cycle comprising daily dosing for 5 days followed by 9 days off treatment."( Phase I study of STX 64 (667 Coumate) in breast cancer patients: the first study of a steroid sulfatase inhibitor.
Coombes, RC; Dobbs, N; Elliott, M; Kulinskaya, E; Potter, BV; Purohit, A; Reed, MJ; Stanczyk, FZ; Stanway, SJ; Sufi, S; Vigushin, D; Ward, R; Wilson, RH; Woo, LW, 2006
)
0.33
"The median inhibition of STS activity by STX64 was 98% in peripheral blood lymphocytes (PBL) and 99% in breast tumor tissue at the end of the 5-day dosing period."( Phase I study of STX 64 (667 Coumate) in breast cancer patients: the first study of a steroid sulfatase inhibitor.
Coombes, RC; Dobbs, N; Elliott, M; Kulinskaya, E; Potter, BV; Purohit, A; Reed, MJ; Stanczyk, FZ; Stanway, SJ; Sufi, S; Vigushin, D; Ward, R; Wilson, RH; Woo, LW, 2006
)
0.33
" Dose-response studies in the same rat model demonstrated that more than 90% inhibition of STS activity in tumors was necessary to induce tumor shrinkage."( A novel steroidal selective steroid sulfatase inhibitor KW-2581 inhibits sulfated-estrogen dependent growth of breast cancer cells in vitro and in animal models.
Akinaga, S; Anazawa, H; Ishida, H; Kuwabara, T; Li, PK; Murakata, C; Nakata, T; Sato, N; Shiotsu, Y; Suzuki, M; Takebayashi, M; Tanaka, H; Terasaki, Y, 2007
)
0.34
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (16)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Carbonic anhydrase 12Homo sapiens (human)Ki54.42450.00021.10439.9000AID1798596; AID365987
Carbonic anhydrase 1Homo sapiens (human)Ki54.68900.00001.372610.0000AID1798596; AID365978
Carbonic anhydrase 2Homo sapiens (human)IC50 (µMol)0.01800.00021.10608.3000AID1796987; AID1797029; AID47745
Carbonic anhydrase 2Homo sapiens (human)Ki54.42520.00000.72369.9200AID1798596; AID365979
Carbonic anhydrase 3Homo sapiens (human)Ki108.26980.00022.010210.0000AID1798596; AID365980
Steryl-sulfataseHomo sapiens (human)IC50 (µMol)0.07550.00010.40717.6000AID1071646; AID1298865; AID1299653; AID1482687; AID1482692; AID1482695; AID1657459; AID1657461; AID1797029; AID1798411; AID1798412; AID1855807; AID1874968; AID1874969; AID1903904; AID291838; AID340415; AID461812; AID623100; AID644202; AID70816; AID71010
AromataseHomo sapiens (human)IC50 (µMol)0.30000.00001.290410.0000AID1798411; AID340414; AID461809
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)IC50 (µMol)0.30000.00071.979812.5000AID461809
Carbonic anhydrase 4Homo sapiens (human)Ki54.42550.00021.97209.9200AID1798596; AID365981
Carbonic anhydrase 6Homo sapiens (human)Ki54.47380.00011.47109.9200AID1798596; AID365984
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki54.48250.00001.27259.9000AID1798596; AID365982
Carbonic anhydrase 7Homo sapiens (human)Ki54.42540.00021.37379.9000AID1798596; AID365985
Carbonic anhydrase 9Homo sapiens (human)Ki54.42620.00010.78749.9000AID1798596; AID365986
Carbonic anhydrase 13Mus musculus (house mouse)Ki54.50440.00021.39749.9000AID1798596; AID365988
Carbonic anhydrase 14Homo sapiens (human)Ki54.48170.00021.50999.9000AID1798596; AID365989
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)Ki54.47900.00001.34129.9700AID1798596; AID365983
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Carbonic anhydrase IIHomo sapiens (human)Kd0.04500.04500.04500.0450AID977611
Carbonic anhydrase 2Homo sapiens (human)Kd0.04500.00000.41575.5500AID1796988
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (38)

Processvia Protein(s)Taxonomy
estrous cycleCarbonic anhydrase 12Homo sapiens (human)
chloride ion homeostasisCarbonic anhydrase 12Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 12Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 1Homo sapiens (human)
morphogenesis of an epitheliumCarbonic anhydrase 2Homo sapiens (human)
positive regulation of synaptic transmission, GABAergicCarbonic anhydrase 2Homo sapiens (human)
positive regulation of cellular pH reductionCarbonic anhydrase 2Homo sapiens (human)
angiotensin-activated signaling pathwayCarbonic anhydrase 2Homo sapiens (human)
regulation of monoatomic anion transportCarbonic anhydrase 2Homo sapiens (human)
secretionCarbonic anhydrase 2Homo sapiens (human)
regulation of intracellular pHCarbonic anhydrase 2Homo sapiens (human)
neuron cellular homeostasisCarbonic anhydrase 2Homo sapiens (human)
positive regulation of dipeptide transmembrane transportCarbonic anhydrase 2Homo sapiens (human)
regulation of chloride transportCarbonic anhydrase 2Homo sapiens (human)
carbon dioxide transportCarbonic anhydrase 2Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 2Homo sapiens (human)
response to bacteriumCarbonic anhydrase 3Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 3Homo sapiens (human)
steroid catabolic processSteryl-sulfataseHomo sapiens (human)
female pregnancySteryl-sulfataseHomo sapiens (human)
epidermis developmentSteryl-sulfataseHomo sapiens (human)
negative regulation of chronic inflammatory responseAromataseHomo sapiens (human)
steroid biosynthetic processAromataseHomo sapiens (human)
estrogen biosynthetic processAromataseHomo sapiens (human)
androgen catabolic processAromataseHomo sapiens (human)
syncytium formationAromataseHomo sapiens (human)
negative regulation of macrophage chemotaxisAromataseHomo sapiens (human)
sterol metabolic processAromataseHomo sapiens (human)
female genitalia developmentAromataseHomo sapiens (human)
mammary gland developmentAromataseHomo sapiens (human)
uterus developmentAromataseHomo sapiens (human)
prostate gland growthAromataseHomo sapiens (human)
testosterone biosynthetic processAromataseHomo sapiens (human)
positive regulation of estradiol secretionAromataseHomo sapiens (human)
female gonad developmentAromataseHomo sapiens (human)
response to estradiolAromataseHomo sapiens (human)
bicarbonate transportCarbonic anhydrase 4Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 4Homo sapiens (human)
detection of chemical stimulus involved in sensory perception of bitter tasteCarbonic anhydrase 6Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 6Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicCarbonic anhydrase 7Homo sapiens (human)
positive regulation of cellular pH reductionCarbonic anhydrase 7Homo sapiens (human)
neuron cellular homeostasisCarbonic anhydrase 7Homo sapiens (human)
regulation of chloride transportCarbonic anhydrase 7Homo sapiens (human)
regulation of intracellular pHCarbonic anhydrase 7Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 7Homo sapiens (human)
response to hypoxiaCarbonic anhydrase 9Homo sapiens (human)
morphogenesis of an epitheliumCarbonic anhydrase 9Homo sapiens (human)
response to xenobiotic stimulusCarbonic anhydrase 9Homo sapiens (human)
response to testosteroneCarbonic anhydrase 9Homo sapiens (human)
secretionCarbonic anhydrase 9Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 9Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 14Homo sapiens (human)
response to bacteriumCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (19)

Processvia Protein(s)Taxonomy
zinc ion bindingCarbonic anhydrase 12Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 12Homo sapiens (human)
arylesterase activityCarbonic anhydrase 1Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 1Homo sapiens (human)
protein bindingCarbonic anhydrase 1Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 1Homo sapiens (human)
hydro-lyase activityCarbonic anhydrase 1Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 1Homo sapiens (human)
arylesterase activityCarbonic anhydrase 2Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 2Homo sapiens (human)
protein bindingCarbonic anhydrase 2Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 2Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 2Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 3Homo sapiens (human)
protein bindingCarbonic anhydrase 3Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 3Homo sapiens (human)
nickel cation bindingCarbonic anhydrase 3Homo sapiens (human)
steryl-sulfatase activitySteryl-sulfataseHomo sapiens (human)
sulfuric ester hydrolase activitySteryl-sulfataseHomo sapiens (human)
metal ion bindingSteryl-sulfataseHomo sapiens (human)
arylsulfatase activitySteryl-sulfataseHomo sapiens (human)
iron ion bindingAromataseHomo sapiens (human)
steroid hydroxylase activityAromataseHomo sapiens (human)
electron transfer activityAromataseHomo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenAromataseHomo sapiens (human)
oxygen bindingAromataseHomo sapiens (human)
heme bindingAromataseHomo sapiens (human)
aromatase activityAromataseHomo sapiens (human)
protein bindingCarbonic anhydrase 4Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 4Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 4Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 6Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 6Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 7Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 7Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 9Homo sapiens (human)
protein bindingCarbonic anhydrase 9Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 9Homo sapiens (human)
molecular function activator activityCarbonic anhydrase 9Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 14Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 14Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (31)

Processvia Protein(s)Taxonomy
plasma membraneCarbonic anhydrase 12Homo sapiens (human)
membraneCarbonic anhydrase 12Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 12Homo sapiens (human)
apical plasma membraneCarbonic anhydrase 12Homo sapiens (human)
plasma membraneCarbonic anhydrase 12Homo sapiens (human)
cytosolCarbonic anhydrase 1Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 1Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
cytosolCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
myelin sheathCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 2Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
cytosolCarbonic anhydrase 3Homo sapiens (human)
cytosolCarbonic anhydrase 3Homo sapiens (human)
cytoplasmCarbonic anhydrase 3Homo sapiens (human)
lysosomeSteryl-sulfataseHomo sapiens (human)
endosomeSteryl-sulfataseHomo sapiens (human)
endoplasmic reticulumSteryl-sulfataseHomo sapiens (human)
endoplasmic reticulum lumenSteryl-sulfataseHomo sapiens (human)
endoplasmic reticulum membraneSteryl-sulfataseHomo sapiens (human)
Golgi apparatusSteryl-sulfataseHomo sapiens (human)
plasma membraneSteryl-sulfataseHomo sapiens (human)
membraneSteryl-sulfataseHomo sapiens (human)
intracellular membrane-bounded organelleSteryl-sulfataseHomo sapiens (human)
endoplasmic reticulumAromataseHomo sapiens (human)
endoplasmic reticulum membraneAromataseHomo sapiens (human)
membraneAromataseHomo sapiens (human)
endoplasmic reticulumAromataseHomo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 4Homo sapiens (human)
rough endoplasmic reticulumCarbonic anhydrase 4Homo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartmentCarbonic anhydrase 4Homo sapiens (human)
Golgi apparatusCarbonic anhydrase 4Homo sapiens (human)
trans-Golgi networkCarbonic anhydrase 4Homo sapiens (human)
plasma membraneCarbonic anhydrase 4Homo sapiens (human)
external side of plasma membraneCarbonic anhydrase 4Homo sapiens (human)
cell surfaceCarbonic anhydrase 4Homo sapiens (human)
membraneCarbonic anhydrase 4Homo sapiens (human)
apical plasma membraneCarbonic anhydrase 4Homo sapiens (human)
transport vesicle membraneCarbonic anhydrase 4Homo sapiens (human)
secretory granule membraneCarbonic anhydrase 4Homo sapiens (human)
brush border membraneCarbonic anhydrase 4Homo sapiens (human)
perinuclear region of cytoplasmCarbonic anhydrase 4Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 4Homo sapiens (human)
plasma membraneCarbonic anhydrase 4Homo sapiens (human)
extracellular regionCarbonic anhydrase 6Homo sapiens (human)
extracellular spaceCarbonic anhydrase 6Homo sapiens (human)
cytosolCarbonic anhydrase 6Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 6Homo sapiens (human)
extracellular spaceCarbonic anhydrase 6Homo sapiens (human)
mitochondrial matrixCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
cytoplasmCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
cytosolCarbonic anhydrase 7Homo sapiens (human)
cytoplasmCarbonic anhydrase 7Homo sapiens (human)
nucleolusCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 9Homo sapiens (human)
membraneCarbonic anhydrase 9Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 9Homo sapiens (human)
microvillus membraneCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 14Homo sapiens (human)
membraneCarbonic anhydrase 14Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 14Homo sapiens (human)
apical plasma membraneCarbonic anhydrase 14Homo sapiens (human)
plasma membraneCarbonic anhydrase 14Homo sapiens (human)
mitochondrionCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
mitochondrial matrixCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
cytoplasmCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (78)

Assay IDTitleYearJournalArticle
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2005The Biochemical journal, Feb-01, Volume: 385, Issue:Pt 3
Crystal structure of human carbonic anhydrase II at 1.95 A resolution in complex with 667-coumate, a novel anti-cancer agent.
AID1811Experimentally measured binding affinity data derived from PDB2005The Biochemical journal, Feb-01, Volume: 385, Issue:Pt 3
Crystal structure of human carbonic anhydrase II at 1.95 A resolution in complex with 667-coumate, a novel anti-cancer agent.
AID1798596CA Inhibition Assay from Article 10.1016/j.bmcl.2008.06.105: \\Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.\\2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
AID1798411Aromatase Inhibition Assay from Article 10.1021/jm800168s: \\Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity.\\2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity.
AID1797029Carbonic Anhydrase Inhibition Assay from Article 10.1016/s0006-291x(03)00865-9: \\Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamates.\\2003Biochemical and biophysical research communications, Jun-13, Volume: 305, Issue:4
Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamates.
AID1798412Sulfatase Inhibition Assay from Article 10.1021/jm800168s: \\Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity.\\2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity.
AID1796988Measurement of Dissociation Constant from Article 10.1021/bi047692e: \\First crystal structures of human carbonic anhydrase II in complex with dual aromatase-steroid sulfatase inhibitors.\\2005Biochemistry, May-10, Volume: 44, Issue:18
First crystal structures of human carbonic anhydrase II in complex with dual aromatase-steroid sulfatase inhibitors.
AID1796987Carbonic Anhydrase Inhibition Assay from Article 10.1021/bi047692e: \\First crystal structures of human carbonic anhydrase II in complex with dual aromatase-steroid sulfatase inhibitors.\\2005Biochemistry, May-10, Volume: 44, Issue:18
First crystal structures of human carbonic anhydrase II in complex with dual aromatase-steroid sulfatase inhibitors.
AID291838Inhibition of steroid sulfatase in JEG3 cell membrane2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Dual aromatase-steroid sulfatase inhibitors.
AID291843Inhibition of steroid sulfatase in Wistar rat assessed as reduction of PMSG-stimulated plasma estradiol level at 10 mg/kg, po after 3 hrs2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Dual aromatase-steroid sulfatase inhibitors.
AID1657461Inhibition of steroid sulfatase in human JEG3 cell lysates using [3H] E1S as substrate after 1 hr by scintillation spectrometry analysis2020Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8
A new series of aryl sulfamate derivatives: Design, synthesis, and biological evaluation.
AID1124821Inhibition of steroid sulfatase in human MCF7 cells assessed as conversion of [3H]E1S to [3H]E1 and [3H]E2 at 1 uM after 5 hrs by liquid scintillation counting2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Design and synthesis of silicon-containing steroid sulfatase inhibitors possessing pro-estrogen antagonistic character.
AID1657459Inhibition of steroid sulfatase in human JEG3 cells using [3H] E1S as substrate incubated for 20 hrs by scintillation spectrometry analysis2020Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8
A new series of aryl sulfamate derivatives: Design, synthesis, and biological evaluation.
AID205773In vitro inhibition of [6,7-3H]E1S binding to steroid sulfatase in JEG-3 human placental carcinoma cells at 3.3 nM2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
First dual aromatase-steroid sulfatase inhibitors.
AID70990Compound was evaluated for its percent inhibition against the estrone sulfatase enzyme at a concentration of 5 uM2002Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES).
AID365980Inhibition of human cloned CA3 by stopped-flow CO2 hydration method2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
AID1299653Inhibition of placental microsomal estrone sulfatase (unknown origin) using [3H]-estrone sulphate as substrate2016European journal of medicinal chemistry, May-23, Volume: 114Sulfatase inhibitors for recidivist breast cancer treatment: A chemical review.
AID1482698Antiproliferative activity against E1S/E1-stimulated human T47D cells assessed as cell viability at 50 to 200 nM measured after 7 days after MTT assay relative to control2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases.
AID1299643Potency index, ratio of EMATE IC50 to compound IC50 for placental microsomal estrone sulfatase (unknown origin)2016European journal of medicinal chemistry, May-23, Volume: 114Sulfatase inhibitors for recidivist breast cancer treatment: A chemical review.
AID1482687Inhibition of human placental microsomal STS assessed as formation of E1 preincubated for 30 mins followed by addition of E1S as substrate measured after 20 mins by ELISA2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases.
AID365981Inhibition of human cloned CA4 by stopped-flow CO2 hydration method2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
AID26348pKa value was determined2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
AID1874970Inhibition of human placental cytosolic fraction 17beta-HSD1 at 1 uM using [3H]-E1 as substrate measured after 10 mins in presence of NADH by HPLC method2022Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17
Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis.
AID1482686Inhibition of 17beta-HSD1 in human T47D cells at 1 uM preincubated for 1 hr followed by addition of [3H]-E1/E1 as substrate measured after 30 mins by HPLC based radio-detection method2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases.
AID461812Inhibition of steroid sulfatase in human JEG3 cells by scintillation spectrometry2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.
AID365989Inhibition of human cloned CA14 by stopped-flow CO2 hydration method2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
AID340415Inhibition of steroid sulfatase activity in human JEG3 cells2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity.
AID1874968Inhibition of STS in human T47D cells using [3H]E1S as substrate measured after 24 hrs by HPLC analysis2022Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17
Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis.
AID1482704Inhibition of 17beta-HSD1 in human T47D cells assessed as [3H]-E2 level at 200 nM after 48 hrs by HPLC based radio-detection method (Rvb = 95.2%)2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases.
AID1071646Inhibition of steroid sulfatase (unknown origin)2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis, structure-activity relationship of iodinated-4-aryloxymethyl-coumarins as potential anti-cancer and anti-mycobacterial agents.
AID365986Inhibition of human cloned CA9 catalytic domain by stopped-flow CO2 hydration method2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
AID1874974Metabolic stability in mouse liver S9 fraction assessed as intrinsic clearance at 1 uM in presence of NADPH measured upto 60 min by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17
Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis.
AID1657460Inhibition of steroid sulfatase in human JEG3 cell lysates at 10 uM using [3H] E1S as substrate after 1 hr by scintillation spectrometry analysis relative to control2020Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8
A new series of aryl sulfamate derivatives: Design, synthesis, and biological evaluation.
AID70847Compound was evaluated for its inhibitory activity against estrone sulfatase enzyme2002Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES).
AID70816Tested for the inhibitory activity against Estrone Sulfatase2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Determination and use of a transition state for the enzyme estrone sulfatase (ES) from a proposed reaction mechanism.
AID1482692Inhibition of STS in human T47D cells preincubated for 1 hr followed by addition of [3H]-E1S/E1S as substrate measured after 24 hrs by HPLC based radio-detection method2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases.
AID1482695Irreversible inhibition of STS in human T47D cells preincubated for 2 hrs followed by compound washout and addition of [3H]-E1S/E1S as substrate measured after 24 hrs by HPLC based radio-detection method2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases.
AID1063491Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production administered 1 hr prior to LPS-challenge measured after 24 hrs by EIA2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
Synthesis of tricyclic fused coumarin sulfonates and their inhibitory effects on LPS-induced nitric oxide and PGE2 productions in RAW 264.7 macrophages.
AID1874973Metabolic stability in human liver S9 fraction assessed as intrinsic clearance at 1 uM in presence of NADPH measured upto 60 min by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17
Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis.
AID365985Inhibition of human cloned CA7 by stopped-flow CO2 hydration method2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
AID1482710Inhibition of human placental cytosolic 17beta-HSD2 at 1 uM using [3H]-E2/E2 substrate and NAD+ after 20 mins by HPLC based radio-detection method2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases.
AID291844Inhibition of steroid sulfatase in Wistar rat assessed as reduction of PMSG-stimulated plasma estradiol level at 10 mg/kg, po after 24 hrs2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Dual aromatase-steroid sulfatase inhibitors.
AID365979Inhibition of human cloned CA2 by stopped-flow CO2 hydration method2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
AID1874972Metabolic stability in mouse liver S9 fraction assessed as half life at 1 uM in presence of NADPH measured upto 60 min by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17
Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis.
AID365982Inhibition of human cloned CA5A by stopped-flow CO2 hydration method2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
AID71010Inhibition of estrone sulfatase2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
AID291841Inhibition of aromatase in Wistar rat assessed as reduction of PMSG-stimulated plasma estradiol level at 10 mg/kg, po after 3 hrs2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Dual aromatase-steroid sulfatase inhibitors.
AID340414Inhibition of aromatase activity in human JEG3 cells2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity.
AID1063481Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production administered 1 hr prior to LPS-challenge measured after 24 hrs by Griess assay2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
Synthesis of tricyclic fused coumarin sulfonates and their inhibitory effects on LPS-induced nitric oxide and PGE2 productions in RAW 264.7 macrophages.
AID1298865Inhibition of steroid sulfatase in human JEG-3 cells assessed as [14C]-Estrone formation using [3H]E1S as substrate2016Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
Design, synthesis, and biological evaluation of new arylamide derivatives possessing sulfonate or sulfamate moieties as steroid sulfatase enzyme inhibitors.
AID71011Inhibitory activity against estrone sulfatase at 0.25 uM (initial screening)2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
AID461809Inhibition of aromatase in human JEG3 cells by scintillation spectrometry2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.
AID291824Inhibition of Estrone sulfatase in human placental microsome2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Thiosemicarbazones of formyl benzoic acids as novel potent inhibitors of estrone sulfatase.
AID1895185Inhibition of lysosome sulfatase (unknown origin) assessed as reduction in fluorescence intensity using 2-(2-Morpholinoethyl)-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)-1H-benzo[de]-isoquinoline-1,3(2H)-dione as s2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
New Protocol-Guided Exploitation of a Lysosomal Sulfatase Inhibitor to Suppress Cell Growth in Glioblastoma Multiforme.
AID365983Inhibition of human cloned CA5B by stopped-flow CO2 hydration method2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
AID1482709Inhibition of human placental cytosolic 17beta-HSD1 at 1 uM using [3H]-E1/E1 substrate and NADH after 10 mins by HPLC based radio-detection method2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases.
AID365988Inhibition of mouse CA13 by stopped-flow CO2 hydration method2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
AID365987Inhibition of human cloned CA12 catalytic domain by stopped-flow CO2 hydration method2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
AID365978Inhibition of human cloned CA1 by stopped-flow CO2 hydration method2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
AID1874969Irreversible inhibition of STS in human T47D cells using [3H]E1S as substrate measured after 24 hrs by HPLC analysis2022Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17
Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis.
AID1482702Inhibition of 17beta-HSD1 in human T47D cells assessed as [3H]-E1 level at 200 nM after 48 hrs by HPLC based radio-detection method (Rvb = 0.9%)2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases.
AID623100Inhibition of steroid sulfatase in human intact MCF7 cells2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Inhibition of steroid sulfatase with 4-substituted estrone and estradiol derivatives.
AID291842Inhibition of aromatase in Wistar rat assessed as reduction of PMSG-stimulated plasma estradiol level at 10 mg/kg, po after 24 hrs2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Dual aromatase-steroid sulfatase inhibitors.
AID1657462Antiproliferative activity against human T47D cells assessed as reduction in cell proliferation measured after 5 days in presence of estradiol sulfate by crystal violet staining based assay2020Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8
A new series of aryl sulfamate derivatives: Design, synthesis, and biological evaluation.
AID1855807Inhibition of STS in human placental microsomes2022European journal of medicinal chemistry, Nov-05, Volume: 241An overview on Estrogen receptors signaling and its ligands in breast cancer.
AID365984Inhibition of human cloned CA6 by stopped-flow CO2 hydration method2008Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
AID1903904Inhibition of STS in human MCF7 cells using [3H]E1S as substrate incubated for 20 hrs by radioisotope cellular assay2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Development of Sulfamoylated 4-(1-Phenyl-1
AID19659Partition coefficient (logP)2002Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES).
AID1903902Inhibition of STS in human MCF7 cells assessed as residual enzyme activity using [3H]E1S as substrate at 10 nM incubated for 20 hrs by radioisotope cellular assay relative to control2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Development of Sulfamoylated 4-(1-Phenyl-1
AID1903903Inhibition of STS in human MCF7 cells assessed as residual enzyme activity using [3H]E1S as substrate at 1 nM incubated for 20 hrs by radioisotope cellular assay relative to control2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Development of Sulfamoylated 4-(1-Phenyl-1
AID291837Inhibition of aromatase in JEG3 cell membrane2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Dual aromatase-steroid sulfatase inhibitors.
AID1874971Metabolic stability in human liver S9 fraction assessed as half life at 1 uM in presence of NADPH measured upto 60 min by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17
Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis.
AID1482700Inhibition of STS in human T47D cells assessed as [3H]-E1S level at 200 nM after 48 hrs by HPLC based radio-detection method (Rvb = 3.9%)2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases.
AID644202Irreversible inhibition of steroid sulfatase in human intact MCF7 cells2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
17β-Arylsulfonamides of 17β-aminoestra-1,3,5(10)-trien-3-ol as highly potent inhibitors of steroid sulfatase.
AID47745Compound was tested for inhibition of human carbonic anhydrase (hCA II)2003Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5
Docking studies of sulphamate inhibitors of estrone sulphatase in human carbonic anhydrase II.
AID1903873Inhibition of STS in human MCF7 cells assessed as residual enzyme activity using [3H]E1S as substrate at 100 nM incubated for 20 hrs by radioisotope cellular assay relative to control2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Development of Sulfamoylated 4-(1-Phenyl-1
AID19447Partition coefficient (logP)2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (66)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's33 (50.00)29.6817
2010's25 (37.88)24.3611
2020's8 (12.12)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 24.81

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index24.81 (24.57)
Research Supply Index4.30 (2.92)
Research Growth Index5.78 (4.65)
Search Engine Demand Index26.67 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (24.81)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (7.35%)5.53%
Reviews9 (13.24%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other54 (79.41%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]