Abstract:
:We report the initial results of our study into the use of a potential transition state (TS) of the reaction catalyzed by the enzyme estrone sulfatase (ES) in the design of a series of simple 4'-O-sulfamoyl-4-biphenyl-based compounds as novel inhibitors of ES. The results of the study show that these compounds are: potent inhibitors, possessing greater inhibitory activity than 4-methylcoumarin-7-O-sulfamate (COUMATE); weaker inhibitors than the tricyclic derivative of COUMATE, namely 667-COUMATE and the steroidal inhibitor estrone-3-O-sulfamate (EMATE), and irreversible inhibitors of ES.
journal_name
Biochem Biophys Res Communjournal_title
Biochemical and biophysical research communicationsauthors
Ahmed S,James K,Owen CPdoi
10.1016/S0006-291X(02)00444-8subject
Has Abstractpub_date
2002-05-31 00:00:00pages
180-3issue
1eissn
0006-291Xissn
1090-2104pii
S0006-291X(02)00444-8journal_volume
294pub_type
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