| Assay ID | Title | Year | Journal | Article |
|---|
| AID70994 | Compound was tested for the Inhibitory activity against the Estrone Sulfatase at a concentration of 50 uM; ND means not determined | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
| Inhibition of estrone sulfatase (ES) by derivatives of 4-[(aminosulfonyl)oxy] benzoic acid. |
| AID69861 | Affinity for human estrogen receptor alpha | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
| 6-(2-adamantan-2-ylidene-hydroxybenzoxazole)-O-sulfamate: a potent non-steroidal irreversible inhibitor of human steroid sulfatase. |
| AID47930 | Inhibition against human carbonic anhydrase II | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
| Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatase. |
| AID205795 | Tested for relative inhibitory potency against recombinant human steroid sulfatase | 2000 | Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
| New fluorogenic substrate for the first continuous steroid sulfatase assay. |
| AID654851 | Inhibition of steroid sulfatase in rat liver at 10 mg/kg, sc administered as single dose measured up to 7 days | 2012 | Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
| Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors. |
| AID1865674 | Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
| Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents. |
| AID1865676 | Inhibition of Arylsulfatase (unknown origin) using potassium p-nitrophenyl sulfate as substrate incubated for 5 mins | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
| Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents. |
| AID70819 | In vitro inhibition of estrone sulfatase in placental microsomes | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
| Synthesis and biological activity of the superestrogen (E)-17-oximino-3-O-sulfamoyl-1,3,5(10)-estratriene: x-ray crystal structure of (E)-17-oximino-3-hydroxy-1,3,5(10)-estratriene. |
| AID47745 | Compound was tested for inhibition of human carbonic anhydrase (hCA II) | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5
| Docking studies of sulphamate inhibitors of estrone sulphatase in human carbonic anhydrase II. |
| AID205757 | Inhibition of steroid sulfatase activity by the compound was determined in human embryonic kidney (HEK)-293 cells transfected with a sulfatase expression vector (pCMV-sulfa) using 100 uM of [3H]E1S | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
| Structure-activity relationships of 17alpha-derivatives of estradiol as inhibitors of steroid sulfatase. |
| AID654849 | Inhibition of steroid sulfatase in rat liver at 10 mg/kg, sc | 2012 | Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
| Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors. |
| AID70193 | Affinity of sulfamate compound for human estrogen receptor alpha | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
| Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase. |
| AID47709 | Inhibition of human recombinant carbonic anhydrase I | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
| Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes I and II and transmembrane, tumor-associated isozyme IX with sulfamates including EMATE also acting as steroid sulfatase inhibitors. |
| AID50344 | Inhibitory activity of compound against human carbonic anhydrase I | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
| Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride. |
| AID654844 | Inhibition of steroid sulfatase in human placental microsomes using [3H]E1S as substrate after 30 mins by scintillation spectrometry | 2012 | Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
| Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors. |
| AID70833 | Tested for inhibition of estrone sulfatase in MCF-7 breast cancer cells using 2 nM substrate concentration at 10 uM | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
| Estrone sulfamates: potent inhibitors of estrone sulfatase with therapeutic potential. |
| AID70844 | In vivo inhibition of estrone sulfatase in rat liver after oral administration | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
| Synthesis and biological activity of the superestrogen (E)-17-oximino-3-O-sulfamoyl-1,3,5(10)-estratriene: x-ray crystal structure of (E)-17-oximino-3-hydroxy-1,3,5(10)-estratriene. |
| AID1249480 | Invivo inhibition of steroid sulfatase activity in rat liver at 10 mg/kg, po measured after 2 hrs | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID1249481 | Invivo inhibition of steroid sulfatase activity in rat liver at 20 mg/kg, po measured after 2 hrs | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID70854 | Inhibitory concentration required to inhibit the enzyme estrone sulfatase was determined | 2002 | Bioorganic & 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). |
| AID291824 | Inhibition of Estrone sulfatase in human placental microsome | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Thiosemicarbazones of formyl benzoic acids as novel potent inhibitors of estrone sulfatase. |
| AID254248 | Inhibition of catalytic domain of human recombinant carbonic anhydrase IX | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Carbonic anhydrase inhibitors: stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II. |
| AID1299672 | Inhibition of human placental microsomal estrone sulfatase using 4-methylumbelliferyl sulfate as substrate incubated for 1 hr by fluorescence assay | 2016 | European journal of medicinal chemistry, May-23, Volume: 114 | Sulfatase inhibitors for recidivist breast cancer treatment: A chemical review. |
| AID257064 | Inhibition of recombinant human mitochondrial isozyme CA VA | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
| Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides. |
| AID70839 | Estrogenic potency against Estrone sulfatase (E1-STS) was determined in vivo by administering to rats | 1996 | Journal of medicinal chemistry, Mar-29, Volume: 39, Issue:7
| Active site directed inhibition of estrone sulfatase by nonsteroidal coumarin sulfamates. |
| AID1299668 | Inhibition of estrone sulfatase in human JEG-3 cells using [3H]-estrone sulphate as substrate incubated for 4 hrs by liquid scintillation counting method | 2016 | European journal of medicinal chemistry, May-23, Volume: 114 | Sulfatase inhibitors for recidivist breast cancer treatment: A chemical review. |
| AID1249487 | Inhibition of STS (unknown origin) at 1 uM | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID103895 | Anti-proliferative activity against MCF-7 human breast cancer cells was determined by using MCF-7 plate assay | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
| 2-Alkylsulfanyl estrogen derivatives: synthesis of a novel class of multi-targeted anti-tumour agents. |
| AID70852 | Inhibitory concentration against estrone sulfatase | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
| Acid dissociation constant, a potential physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES). |
| AID205782 | Rate constant of inactivation against human steroid sulfatase | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
| 6-(2-adamantan-2-ylidene-hydroxybenzoxazole)-O-sulfamate: a potent non-steroidal irreversible inhibitor of human steroid sulfatase. |
| AID1865675 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
| Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents. |
| AID19447 | Partition coefficient (logP) | 2004 | Bioorganic & 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. |
| AID55980 | In vivo inhibition against dehydroepiandrosterone sulfatase (DHA-STS) in rat liver. | 1996 | Journal of medicinal chemistry, Mar-29, Volume: 39, Issue:7
| Active site directed inhibition of estrone sulfatase by nonsteroidal coumarin sulfamates. |
| AID1600013 | In vivo inhibition of liver steroid sulfatase in Wistar rat at 0.1 mg/kg relative to control | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Sulfamates in drug design and discovery: Pre-clinical and clinical investigations. |
| AID1865672 | Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
| Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents. |
| AID102630 | Stimulation of MCF-7 cell proliferation at 1000 nM | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
| Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase. |
| AID26792 | Partition coefficient (logP) | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18
| Hydrophobicity, a physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES). |
| AID102628 | Stimulation of MCF-7 cell proliferation at 100 nM | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
| Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase. |
| AID26348 | pKa value was determined | 2004 | Bioorganic & 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. |
| AID654845 | Inhibition of steroid sulfatase in human MCF7 cells using [3H]E1S as substrate after 20 hrs by scintillation spectrometry | 2012 | Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
| Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors. |
| AID70851 | Inhibition of Estrone sulfatase | 2001 | Bioorganic & medicinal chemistry letters, Mar-26, Volume: 11, Issue:6
| Novel inhibitors of the enzyme estrone sulfatase (ES). |
| AID70838 | Inhibition of estrone sulfatase in MCF-7 breast cancer cells at 0.1 uM | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
| Synthesis and biological activity of the superestrogen (E)-17-oximino-3-O-sulfamoyl-1,3,5(10)-estratriene: x-ray crystal structure of (E)-17-oximino-3-hydroxy-1,3,5(10)-estratriene. |
| AID1865670 | Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
| Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents. |
| AID48298 | Inhibition against human carbonic anhydrase IX | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
| Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatase. |
| AID1865671 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
| Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents. |
| AID238668 | Inhibitory activity against human steroid sulfatase | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
| 2-(1-adamantyl)-4-(thio)chromenone-6-carboxylic acids: potent reversible inhibitors of human steroid sulfatase. |
| AID70829 | Tested for enzyme inhibition after 20h in MCF-7 breast cancer cells at 1 uM; NA=No activity | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
| Estrone sulfamates: potent inhibitors of estrone sulfatase with therapeutic potential. |
| AID1299647 | Inhibition of estrone sulfatase (unknown origin) transfected in HEK293 cells using [3H]E1S as substrate incubated for 2 hrs by liquid scintillation counting method | 2016 | European journal of medicinal chemistry, May-23, Volume: 114 | Sulfatase inhibitors for recidivist breast cancer treatment: A chemical review. |
| AID205766 | Inhibitory activity against purified human Steroid sulfatase | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
| Nortropinyl-arylsulfonylureas as novel, reversible inhibitors of human steroid sulfatase. |
| AID48305 | Inhibitory concentration against catalytic domain of human cloned carbonic anhydrase IX. | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
| Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes I and II and transmembrane, tumor-associated isozyme IX with sulfamates including EMATE also acting as steroid sulfatase inhibitors. |
| AID205770 | Inhibitory activity against steroid sulfatase enzyme | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
| 2-Alkylsulfanyl estrogen derivatives: synthesis of a novel class of multi-targeted anti-tumour agents. |
| AID1249553 | Invivo inhibition of steroid sulfatase activity in human assessed as decrease in DHEA level after 72 hrs | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID47748 | Inhibitory activity of compound against human carbonic anhydrase II | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
| Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride. |
| AID1249484 | Invivo inhibition of steroid sulfatase activity in rat WBC at 20 mg/kg, po measured after 2 hrs | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID241794 | Inhibitory concentration against human steroid sulfatase expressed in CHO cells | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
| N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase. |
| AID1438381 | Inhibition of STS in human MCF7 cells | 2017 | European journal of medicinal chemistry, Mar-10, Volume: 128 | Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors. |
| AID1337728 | Inhibition of recombinant human CYP1B1 expressed in bacterial microsomes co-expressing P450 reductase at 3 uM using 7-ethyl-O-resorufin as substrate after 45 mins in presence of NADPH by fluorescence assay relative to control | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Targeting cytochrome P450 (CYP) 1B1 with steroid derivatives. |
| AID70019 | Affinity for human estrogen receptor beta | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
| 6-(2-adamantan-2-ylidene-hydroxybenzoxazole)-O-sulfamate: a potent non-steroidal irreversible inhibitor of human steroid sulfatase. |
| AID654850 | Inhibition of steroid sulfatase in rat liver at 10 mg/kg, po administered as single dose measured up to 7 days | 2012 | Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
| Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors. |
| AID48113 | Inhibitory activity of compound against bovine carbonic anhydrase IV; not tested | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
| Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride. |
| AID70816 | Tested for the inhibitory activity against Estrone Sulfatase | 2001 | Bioorganic & 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. |
| AID1249485 | Invivo inhibition of steroid sulfatase activity in rat WBC at 40 mg/kg, po measured after 2 hrs | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID1249555 | Invivo inhibition of steroid sulfatase activity in human assessed as decrease in DHEAS level after 72 hrs | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID248500 | Inhibitory activity against human steroid sulfatase over-expressed in CHO cells | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
| 2-(1-adamantyl)-4-(thio)chromenone-6-carboxylic acids: potent reversible inhibitors of human steroid sulfatase. |
| AID70848 | Inhibitory activity against estrone sulfatase enzyme | 1999 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
| Derivation of a possible transition-state for the reaction catalysed by the enzyme estrone Sulfatase (ES). |
| AID275898 | Inhibition of human CA2 | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
| 2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity. |
| AID70509 | Affinity of sulfamate compound for human estrogen receptor beta | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
| Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase. |
| AID70840 | In vivo inhibition against Estrone sulfatase (E1-STS) in rat liver. | 1996 | Journal of medicinal chemistry, Mar-29, Volume: 39, Issue:7
| Active site directed inhibition of estrone sulfatase by nonsteroidal coumarin sulfamates. |
| AID461822 | Inhibition of human CA2 by colorimetric assay | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
| Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template. |
| AID1299670 | Inhibition of human placental microsomal estrone sulfatase using [3H]E1S as substrate incubated for 20 mins by scintillation counting method | 2016 | European journal of medicinal chemistry, May-23, Volume: 114 | Sulfatase inhibitors for recidivist breast cancer treatment: A chemical review. |
| AID205762 | Inhibitory activity against Steroid sulfatase expressed in CHO cells | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
| Nortropinyl-arylsulfonylureas as novel, reversible inhibitors of human steroid sulfatase. |
| AID1243900 | Inhibition of STS in human MCF7 cells | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors. |
| AID1299642 | Inhibition of placental microsomal estrone sulfatase (unknown origin) using [6,7-3H]E1S as substrate incubated for 1 hr by scintillation spectrometric analysis | 2016 | European journal of medicinal chemistry, May-23, Volume: 114 | Sulfatase inhibitors for recidivist breast cancer treatment: A chemical review. |
| AID205769 | Inhibition of steroid sulfatase | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
| Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase. |
| AID1249554 | Invivo inhibition of steroid sulfatase activity in human assessed as decrease in DHEAS level after 24 hrs | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID654848 | Inhibition of steroid sulfatase in rat liver at 10 mg/kg, po | 2012 | Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
| Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors. |
| AID70849 | Inhibitory activity against Estrone Sulfatase | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
| Inhibition of estrone sulfatase (ES) by derivatives of 4-[(aminosulfonyl)oxy] benzoic acid. |
| AID71010 | Inhibition of estrone sulfatase | 2004 | Bioorganic & 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. |
| AID1249479 | Invivo inhibition of steroid sulfatase activity in Wistar rat liver assessed as inhibition of dehydroepiandrosterone sulfate hydrolysis at 0.1 mg/kg, sc for 7 days | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID19659 | Partition coefficient (logP) | 2002 | Bioorganic & 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). |
| AID70831 | Tested for inhibition of estrone sulfatase in MCF-7 breast cancer cells using 2 nM substrate concentration at 1 uM | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
| Estrone sulfamates: potent inhibitors of estrone sulfatase with therapeutic potential. |
| AID240903 | Inhibition of purified human steroid sulfatase | 2004 | Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
| Estrone formate: a novel type of irreversible inhibitor of human steroid sulfatase. |
| AID71012 | Inhibitory activity against estrone sulfatase at 10 uM (initial screening) | 2004 | Bioorganic & 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. |
| AID190399 | Effect on uterine weight gain in ovariectomized rat, expressed as uterine weight/total body weight X100 (0.036+/-0.001) | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
| Synthesis and biological activity of the superestrogen (E)-17-oximino-3-O-sulfamoyl-1,3,5(10)-estratriene: x-ray crystal structure of (E)-17-oximino-3-hydroxy-1,3,5(10)-estratriene. |
| AID1249482 | Invivo inhibition of steroid sulfatase activity in rat liver at 40 mg/kg, po measured after 2 hrs | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID70837 | Inhibitory activity against Estrone sulfatase (E1-STS) in MCF-7 breast cancer cells at 0.1 uM | 1996 | Journal of medicinal chemistry, Mar-29, Volume: 39, Issue:7
| Active site directed inhibition of estrone sulfatase by nonsteroidal coumarin sulfamates. |
| AID70824 | Tested for inhibition of estrone sulfatase in placental microsomal preparation (100000 g pellet) using substrate concentration of 20 uM | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
| Estrone sulfamates: potent inhibitors of estrone sulfatase with therapeutic potential. |
| AID205779 | Inhibitory constant against human steroid sulfatase in CHO cells | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
| 6-(2-adamantan-2-ylidene-hydroxybenzoxazole)-O-sulfamate: a potent non-steroidal irreversible inhibitor of human steroid sulfatase. |
| AID1249494 | Inhibition of human carbonic anhydrase 2 | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID70857 | Compound was evaluated for its percent inhibition against the enzyme estrone sulfatase | 2002 | Bioorganic & 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). |
| AID1299666 | Inhibition of human placental estrone sulfatase expressed in HEK293 cells using [3H]E1S as substrate incubated for 2 hrs by liquid scintillation counting method | 2016 | European journal of medicinal chemistry, May-23, Volume: 114 | Sulfatase inhibitors for recidivist breast cancer treatment: A chemical review. |
| AID1249476 | Inhibition of STS activity in human MCF7 cells at 0.1 uM | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID644086 | Inhibition of human carbonic anhydrase 4 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Structure-activity relationships for the interaction of 5,10-dihydroindeno[1,2-b]indole derivatives with human and bovine carbonic anhydrase isoforms I, II, III, IV and VI. |
| AID205754 | Compound was tested for its ability to inhibit the transformation of [C14]-DHEAS to DHEA by steroid sulfatase derived from human embryonal kidney cell | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
| Potent inhibition of steroid sulfatase activity by 3-O-sulfamate 17alpha-benzyl(or 4'-tert-butylbenzyl)estra-1,3,5(10)-trienes: combination of two substituents at positions C3 and c17alpha of estradiol. |
| AID70830 | Tested for inhibition of estrone sulfatase in MCF-7 breast cancer cells using 2 nM substrate concentration at 0.1 uM | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
| Estrone sulfamates: potent inhibitors of estrone sulfatase with therapeutic potential. |
| AID257065 | Inhibition of cloned human transmembrane, tumor-associated isozyme CA IX | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
| Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides. |
| AID1600037 | Inhibition of human placental steroid sulfatase expressed in HEK293 cells using [3H] E1S as substrate after 2 hrs by liquid scintillation counting method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Sulfamates in drug design and discovery: Pre-clinical and clinical investigations. |
| AID238712 | Inhibitory constant against human steroid sulfatase | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
| N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase. |
| AID71005 | Relative potency compared to COUMATE against Estrone sulfatase | 2001 | Bioorganic & medicinal chemistry letters, Mar-26, Volume: 11, Issue:6
| Novel inhibitors of the enzyme estrone sulfatase (ES). |
| AID623099 | Inhibition of human purified steroid sulfatase | 2011 | Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
| Inhibition of steroid sulfatase with 4-substituted estrone and estradiol derivatives. |
| AID644084 | Inhibition of human carbonic anhydrase 1 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Structure-activity relationships for the interaction of 5,10-dihydroindeno[1,2-b]indole derivatives with human and bovine carbonic anhydrase isoforms I, II, III, IV and VI. |
| AID70999 | Inhibitory activity against estrone sulfatase expressed as potency | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18
| Hydrophobicity, a physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES). |
| AID70818 | Inhibitory activity againist Estrone sulfatase from MCF-7 cells (placental microsomes) | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| A novel type of nonsteroidal estrone sulfatase inhibitors. |
| AID1249478 | Invivo inhibition of steroid sulfatase activity in Wistar rat liver assessed as inhibition of estrone sulfate hydrolysis at 0.1 mg/kg, sc for 7 days | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID257063 | Inhibition of recombinant human cytosolic isozyme CA II | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
| Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides. |
| AID1600011 | Inhibition of steroid sulfatase (unknown origin) at 0.1 uM relative to control | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Sulfamates in drug design and discovery: Pre-clinical and clinical investigations. |
| AID1865673 | Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
| Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents. |
| AID205758 | Inhibition of steroid sulfatase activity by the compound was determined in human embryonic kidney (HEK)-293 cells transfected with a sulfatase expression vector (pCMV-sulfa) using 100 uM of [14C]-DHEAS | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
| Structure-activity relationships of 17alpha-derivatives of estradiol as inhibitors of steroid sulfatase. |
| AID644088 | Inhibition of bovine carbonic anhydrase 3 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Structure-activity relationships for the interaction of 5,10-dihydroindeno[1,2-b]indole derivatives with human and bovine carbonic anhydrase isoforms I, II, III, IV and VI. |
| AID70998 | In vitro inhibition of estrone sulfatase at 1 mM. | 2002 | Bioorganic & medicinal chemistry letters, May-06, Volume: 12, Issue:9
| The mechanism of the irreversible inhibition of estrone sulfatase (ES) through the consideration of a range of methane- and amino-sulfonate-based compounds. |
| AID71000 | Inhibitory activity against estrone sulfatase relative to 4-Methylcoumarin-7-O-sulfamate derivative (COUMATE) | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18
| Hydrophobicity, a physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES). |
| AID70847 | Compound was evaluated for its inhibitory activity against estrone sulfatase enzyme | 2002 | Bioorganic & 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). |
| AID1903876 | Inhibition of STS in human MCF7 cells assessed as reduction in [3H]estradiol and [3H]estrone formation using [3H]estrone sulfate as substrate incubated for 20 hrs | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
| Development of Sulfamoylated 4-(1-Phenyl-1 |
| AID1600015 | In vivo inhibition of steroid sulfatase in Wistar rat assessed as enzyme recovery at 10 mg/kg, sc single dose treated for 10 days measured after 15 days relative to control | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Sulfamates in drug design and discovery: Pre-clinical and clinical investigations. |
| AID1600012 | Inhibition of steroid sulfatase (unknown origin) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Sulfamates in drug design and discovery: Pre-clinical and clinical investigations. |
| AID19203 | Calculated partition coefficient (clogP) | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
| Inhibition of estrone sulfatase (ES) by derivatives of 4-[(aminosulfonyl)oxy] benzoic acid. |
| AID71003 | Relative potency against Estrone sulfatase | 2001 | Bioorganic & medicinal chemistry letters, Mar-26, Volume: 11, Issue:6
| Novel inhibitors of the enzyme estrone sulfatase (ES). |
| AID1249552 | Invivo inhibition of steroid sulfatase activity in human assessed as decrease in DHEA level after 12 hrs | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID1299653 | Inhibition of placental microsomal estrone sulfatase (unknown origin) using [3H]-estrone sulphate as substrate | 2016 | European journal of medicinal chemistry, May-23, Volume: 114 | Sulfatase inhibitors for recidivist breast cancer treatment: A chemical review. |
| AID654852 | Inhibition of steroid sulfatase in human placental microsomes | 2012 | Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
| Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors. |
| AID1249492 | Inhibition of STS activity in human placental microsome | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID1667478 | Reversible inhibition of steroid sulfatase in human JEG3 cells using [3H] E1S as substrate by scintillation counting method | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
| Design and synthesis of dansyl-labeled inhibitors of steroid sulfatase for optical imaging. |
| AID254247 | Inhibition of cloned human carbonic anhydrase II | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
| Carbonic anhydrase inhibitors: stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II. |
| AID1249500 | Growth inhibition of human MCF7 cells | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID644087 | Inhibition of human carbonic anhydrase 6 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Structure-activity relationships for the interaction of 5,10-dihydroindeno[1,2-b]indole derivatives with human and bovine carbonic anhydrase isoforms I, II, III, IV and VI. |
| AID205787 | Tested for inhibitory potency against recombinant human steroid sulfatase | 2000 | Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
| New fluorogenic substrate for the first continuous steroid sulfatase assay. |
| AID257062 | Inhibition of recombinant human cytosolic isozyme CA I | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
| Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides. |
| AID205768 | Inhibitory activity against purified human steroid sulfatase (STS) | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
| 2-Substituted 4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase. |
| AID70991 | Compound was tested for the Inhibitory activity against the Estrone Sulfatase at a concentration of 10 uM | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
| Inhibition of estrone sulfatase (ES) by derivatives of 4-[(aminosulfonyl)oxy] benzoic acid. |
| AID644085 | Inhibition of human carbonic anhydrase 2 using 4-nitrophenylacetate as substrate after 3 mins using spectrophotometry by Lineweaver-Burk plot analysis | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Structure-activity relationships for the interaction of 5,10-dihydroindeno[1,2-b]indole derivatives with human and bovine carbonic anhydrase isoforms I, II, III, IV and VI. |
| AID102627 | Stimulation of MCF-7 cell proliferation at 10 nM | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
| Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase. |
| AID1895185 | Inhibition 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 s | 2021 | Journal 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. |
| AID70853 | Inhibition of estrone sulfatase (ES) | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18
| Hydrophobicity, a physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES). |
| AID234881 | Potency for the inhibition of estrone sulfatase relative to coumate | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
| Acid dissociation constant, a potential physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES). |
| AID241447 | Inhibitory concentration against steroid sulfatase in placental microsomes | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
| A-ring-substituted estrogen-3-O-sulfamates: potent multitargeted anticancer agents. |
| AID1600016 | In vivo inhibition of steroid sulfatase in rat at 10 to 40 mg/kg, po relative to control | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Sulfamates in drug design and discovery: Pre-clinical and clinical investigations. |
| AID48092 | Inhibition of human carbonic anhydrase II | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
| Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes I and II and transmembrane, tumor-associated isozyme IX with sulfamates including EMATE also acting as steroid sulfatase inhibitors. |
| AID1249483 | Invivo inhibition of steroid sulfatase activity in rat WBC at 10 mg/kg, po measured after 2 hrs | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
| AID241450 | Inhibitory concentration against human steroid sulfatase | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
| N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase. |
| AID91648 | Inhibition of human steroid sulfatase compared to EMATE | 2002 | Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
| 4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase. |
| AID1865677 | Inhibition of pig brain tubulin polymerization by spectrophotometric method | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
| Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents. |
| AID205780 | Inhibitory constant against purified human Steroid sulfatase | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
| Nortropinyl-arylsulfonylureas as novel, reversible inhibitors of human steroid sulfatase. |
| AID70855 | In vitro inhibition of estrone sulfatase. | 2002 | Bioorganic & medicinal chemistry letters, May-06, Volume: 12, Issue:9
| The mechanism of the irreversible inhibition of estrone sulfatase (ES) through the consideration of a range of methane- and amino-sulfonate-based compounds. |
| AID205639 | Compound was tested for its ability to inhibit human embryonal kidney cell derived steroid sulfatase activity in transforming [3H]E1S (estrone sulfate) to E1 | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
| Potent inhibition of steroid sulfatase activity by 3-O-sulfamate 17alpha-benzyl(or 4'-tert-butylbenzyl)estra-1,3,5(10)-trienes: combination of two substituents at positions C3 and c17alpha of estradiol. |
| AID50365 | Inhibition against human carbonic anhydrase I | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
| Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatase. |
| AID1600014 | In vivo inhibition of steroid sulfatase in Wistar rat assessed as enzyme recovery at 10 mg/kg, sc single dose treated for 3 days measured after 1 week relative to control | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Sulfamates in drug design and discovery: Pre-clinical and clinical investigations. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |