Novel inhibitors of the enzyme estrone sulfatase (ES).
We report the initial results of our study into a series of simple 4-sulfamated phenyl alkyl ketones as potential inhibitors of the enzyme estrone sulfatase. The results of the study show that these compounds are potent inhibitors, possessing greater inhibitory activity than COUMATE, but weaker activity than EMATE. Furthermore, the compounds are observed to be irreversible inhibitors.
School of Chemical and Pharmaceutical Sciences, Kingston University, Kingston upon Thames, Surrey, UK. ch_s534@kingston.ac.uk
S
S
Ahmed
K
K
James
C P
CP
Owen
C K
CK
Patel
M
M
Patel
D000473:Alkanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D003374:Coumarins / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004970:Estrone / Q000031:analogs & derivatives / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007659:Ketones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008698:Mesylates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013429:Sulfatases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013449:Sulfonamides / Q000494:pharmacology; D013451:Sulfonic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
C429426:2-Tetradecylbutane-1,4-diol dimethanesulphonate; C100463:4-methylcoumarin 7-O-sulfamate; D000473:Alkanes; D003374:Coumarins; D004791:Enzyme Inhibitors; D007659:Ketones; D008698:Mesylates; D013449:Sulfonamides; D013451:Sulfonic Acids; C088768:estrone-3-O-sulfamate; D004970:Estrone; C005741:sulfamic acid; D013429:Sulfatases; C020121:estrone sulfatase