Woo, L. W. Lawrence published the artcileDual Aromatase-Steroid Sulfatase Inhibitors, Name: 3-Chloro-4-hydroxy-5-methoxybenzoic acid, the main research area is YM511 sulfamate analog preparation structure aromatase steroid sulfatase inhibitor.
By introducing the steroid sulfatase inhibitory pharmacophore into aromatase inhibitor 1 (YM511), two series of single agent dual aromatase-sulfatase inhibitors (DASIs) were generated. Two best DASIs (I and II) in vitro (JEG-3 cells) had IC50(aromatase) = 0.82 nM; IC50(sulfatase) = 39 nM, and IC50(aromatase) = 0.77 nM; IC50(sulfatase) = 590 nM, resp. X-ray crystallog. of I, and docking studies of selected compounds into an aromatase homol. model and the steroid sulfatase crystal structure are presented. Both I and II inhibit aromatase and sulfatase in PMSG pretreated adult female Wistar rats potently 3 h after a single oral 10 mg/kg dose. Almost complete dual inhibition is observed for I but the levels were reduced to 85% (aromatase) and 72% (sulfatase) after 24 h. DASI I did not inhibit aldosterone synthesis. The development of a potent and selective DASI should allow the therapeutic potential of dual aromatase-sulfatase inhibition in hormone-dependent breast cancer to be assessed.
Journal of Medicinal Chemistry published new progress about Aromatase inhibitors. 62936-23-6 belongs to class chlorides-buliding-blocks, name is 3-Chloro-4-hydroxy-5-methoxybenzoic acid, and the molecular formula is C8H7ClO4, Name: 3-Chloro-4-hydroxy-5-methoxybenzoic acid.
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