title: Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES).
abstract: We report the initial results of our study into a series of simple 4'-O-sulfamoyl-4-biphenyl based compounds as novel inhibitors of the enzyme estrone sulfatase (ES). The results of the study show that these compounds are potent inhibitors, possessing greater inhibitory activity than COUMATE, but weaker inhibitory activity than EMATE or the tricyclic derivative of COUMATE, namely 667-COUMATE. Furthermore, the compounds are observed to be irreversible inhibitors.
authors: School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, KT1 2EE, Surrey, UK. s.ahmed@kingston.ac.uk
authors: Sabbir
authors: S
authors: Ahmed
authors: Karen
authors: K
authors: James
authors: Caroline P
authors: CP
authors: Owen
authors: Chirag K
authors: CK
authors: Patel
mesh_terms: D003374:Coumarins / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D013429:Sulfatases / Q000037:antagonists & inhibitors*; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology; D013451:Sulfonic Acids
chemical_list: D003374:Coumarins; D004791:Enzyme Inhibitors; D013449:Sulfonamides; D013451:Sulfonic Acids; C520511:irosustat; D013429:Sulfatases; C020121:estrone sulfatase