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Literature summary for 3.1.6.2 extracted from

  • Woo, L.W.; Bubert, C.; Sutcliffe, O.B.; Smith, A.; Chander, S.K.; Mahon, M.F.; Purohit, A.; Reed, M.J.; Potter, B.V.
    Dual aromatase-steroid sulfatase inhibitors (2007), J. Med. Chem., 50, 3540-3560.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitor sulfamic acid 2-bromo-4-[[(4-cyanophenyl)[1,2,4]triazol-4-ylamino]methyl]phenyl ester Homo sapiens
in complex with inhibitor sulfamic acid 2-bromo-4-[[(4-cyanophenyl)[1,2,4]triazol-4-ylamino]methyl]phenyl ester Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
sulfamic acid 2-bromo-4-[[(4-cyanophenyl)[1,2,4]triazol-4-ylamino]methyl]phenyl ester dual aromatase-sulfatase inhibitor, IC50 value for aromatase 0.82 nM Homo sapiens
sulfamic acid 2-bromo-4-[[(4-cyanophenyl)[1,2,4]triazol-4-ylamino]methyl]phenyl ester dual aromatase-sulfatase inhibitor. Alomst complete inhibition of both aromates and sulfatase in pregnant mare's serum gonadotropin pretreated female rats 3 h after a single oral dose. No inhibition of aldosterone synthesis Rattus norvegicus
sulfamic acid 5-[[(4-cyanophenyl)[1,2,4]triazol-4-ylamino]-methyl]-2-fluorophenyl ester dual aromatase-sulfatase inhibitor, IC50 value for aromatase 0.77 nM Homo sapiens
sulfamic acid 5-[[(4-cyanophenyl)[1,2,4]triazol-4-ylamino]-methyl]-2-fluorophenyl ester dual aromatase-sulfatase inhibitor. Potent inhibition of both aromates and sulfatase in pregnant mare's serum gonadotropin pretreated female rats 3 h after a single oral dose Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus
-
-
-

Source Tissue

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000039
-
-
Homo sapiens sulfamic acid 2-bromo-4-[[(4-cyanophenyl)[1,2,4]triazol-4-ylamino]methyl]phenyl ester
0.00059
-
-
Homo sapiens sulfamic acid 5-[[(4-cyanophenyl)[1,2,4]triazol-4-ylamino]-methyl]-2-fluorophenyl ester