Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
In our search for potent inhibitors of the enzyme estrone sulfatase (ES), we have undertaken the synthesis and biochemical evaluation of a range of esters of 4-[(aminosulfonyl)oxy] benzoic acid. The results of the study show that the synthesised compounds possess potent inhibitory activity, indeed the cyclooctyl derivative was found to be more potent than 667-COUMATE, which is currently undergoing clinical trials.
Patel
Chirag K
CK
Department of Pharmacy, School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK.
Owen
Caroline P
CP
Ahmed
Sabbir
S
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D019817:Benzoic Acid / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003374:Coumarins / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D004952:Esters; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship; D013429:Sulfatases / Q000037:antagonists & inhibitors*; D013449:Sulfonamides / Q000494:pharmacology; D013451:Sulfonic Acids
D000970:Antineoplastic Agents; D003374:Coumarins; D004791:Enzyme Inhibitors; D004952:Esters; D013449:Sulfonamides; D013451:Sulfonic Acids; C520511:irosustat; D019817:Benzoic Acid; C005741:sulfamic acid; D013429:Sulfatases; C020121:estrone sulfatase