Inhibition of estrone sulfatase (ES) by 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 straight chain alkyl esters of 4-[(aminosulfonyl)oxy] benzoic acid. The results of the study show that the synthesised compounds possess greater inhibitory activity when compared to COUMATE, although they were all found to possess lower inhibitory activity with respect to EMATE. Furthermore, the data suggest a strong correlation between logP and IC(50) and therefore adds further support to our previous report where we suggested a link between inhibitory activity and hydrophobicity.
Ahmed
Sabbir
S
School of Chemical and Pharmaceutical Sciences, Kingston University, Kingston upon Thames, Surrey, UK. ch_s534@kingston.ac.uk
James
Karen
K
Owen
Caroline P
CP
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001565:Benzoates / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship; D013429:Sulfatases / Q000037:antagonists & inhibitors*
D000970:Antineoplastic Agents; D001565:Benzoates; D013429:Sulfatases; C020121:estrone sulfatase