Synthesis, In Vitro Activity and Rationalisation of a Series of Dialkyl Esters of 5-Aminosulfonylisophthanoate as Potential Estrone Sulfatase (ES) Inhibitors

Sabbir Ahmed; Chirag K. Patel

Synthesis, In Vitro Activity and Rationalisation of a Series of Dialkyl Esters of 5-Aminosulfonylisophthanoate as Potential Estrone Sulfatase (ES) Inhibitors

Sabbir Ahmed, Chirag K. Patel

University of the West of Scotland

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

Abstract

We consider dialkyl esters of 5-aminosulfonylisophthanoate-based compounds in our efforts to determine factors involved in determining the overall inhibitory activity against estrone sulfatase (ES). We propose that the weak inhibition observed is due to the increased electron density in the area of the phenyl ring close to the sulfamate moiety.

Original language	English
Pages (from-to)	437-443
Number of pages	7
Journal	Letters in Drug Design & Discovery
Volume	11
Issue number	4
Publication status	Published - 1 May 2014
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

estrone sulfatase
irreversible
inhibition
breast cancer
isophthanoic acid esters
electron density
ES inhibitor

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title = "Synthesis, In Vitro Activity and Rationalisation of a Series of Dialkyl Esters of 5-Aminosulfonylisophthanoate as Potential Estrone Sulfatase (ES) Inhibitors",

abstract = "We consider dialkyl esters of 5-aminosulfonylisophthanoate-based compounds in our efforts to determine factors involved in determining the overall inhibitory activity against estrone sulfatase (ES). We propose that the weak inhibition observed is due to the increased electron density in the area of the phenyl ring close to the sulfamate moiety.",

keywords = "estrone sulfatase, irreversible, inhibition, breast cancer, isophthanoic acid esters, electron density, ES inhibitor",

author = "Sabbir Ahmed and Patel, \{Chirag K.\}",

year = "2014",

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journal = "Letters in Drug Design \& Discovery",

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T1 - Synthesis, In Vitro Activity and Rationalisation of a Series of Dialkyl Esters of 5-Aminosulfonylisophthanoate as Potential Estrone Sulfatase (ES) Inhibitors

AU - Ahmed, Sabbir

AU - Patel, Chirag K.

PY - 2014/5/1

Y1 - 2014/5/1

N2 - We consider dialkyl esters of 5-aminosulfonylisophthanoate-based compounds in our efforts to determine factors involved in determining the overall inhibitory activity against estrone sulfatase (ES). We propose that the weak inhibition observed is due to the increased electron density in the area of the phenyl ring close to the sulfamate moiety.

AB - We consider dialkyl esters of 5-aminosulfonylisophthanoate-based compounds in our efforts to determine factors involved in determining the overall inhibitory activity against estrone sulfatase (ES). We propose that the weak inhibition observed is due to the increased electron density in the area of the phenyl ring close to the sulfamate moiety.

KW - estrone sulfatase

KW - irreversible

KW - inhibition

KW - breast cancer

KW - isophthanoic acid esters

KW - electron density

KW - ES inhibitor

M3 - Article

SN - 1570-1808

VL - 11

SP - 437

EP - 443

JO - Letters in Drug Design & Discovery

JF - Letters in Drug Design & Discovery

IS - 4

ER -

Synthesis, In Vitro Activity and Rationalisation of a Series of Dialkyl Esters of 5-Aminosulfonylisophthanoate as Potential Estrone Sulfatase (ES) Inhibitors

Abstract

UN SDGs

Keywords

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