The design, synthesis, and biochemical evaluation of derivatives of biphenyl sulfamate-based compounds as novel inhibitors of estrone sulfatase.

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.

authors

Ahmed S,James K,Owen CP

doi

10.1016/S0006-291X(02)00444-8

subject

Has Abstract

pub_date

2002-05-31 00:00:00

pages

180-3

issue

1

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(02)00444-8

journal_volume

294

pub_type

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