Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES)

Sabbir Ahmed; Karen James; Caroline P. Owen; Chirag K. Patel

doi:10.1016/S0960-894X(02)00170-1

Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES)

Sabbir Ahmed, Karen James, Caroline P. Owen, Chirag K. Patel

Research output: Contribution to journal › Article › peer-review

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.

Original language	English
Pages (from-to)	1343-1346
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	12
Issue number	10
DOIs	https://doi.org/10.1016/S0960-894X(02)00170-1
Publication status	Published - 20 May 2002

Keywords

nonsteroidal inhibitors
steroid sulfatase
Chemistry

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10.1016/S0960-894X(02)00170-1

http://dx.doi.org/10.1016/S0960-894X(02)00170-1

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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.",

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AU - Ahmed, Sabbir

AU - James, Karen

AU - Owen, Caroline P.

AU - Patel, Chirag K.

PY - 2002/5/20

Y1 - 2002/5/20

N2 - 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.

AB - 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.

KW - nonsteroidal inhibitors

KW - steroid sulfatase

KW - Chemistry

UR - http://www.ncbi.nlm.nih.gov/pubmed/11992773

U2 - 10.1016/S0960-894X(02)00170-1

DO - 10.1016/S0960-894X(02)00170-1

M3 - Article

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SN - 0960-894X

VL - 12

SP - 1343

EP - 1346

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 10

ER -

Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES)

Abstract

Keywords

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