Synthesis, Biological Evaluation and the Rationalisation of the Inhibitory Activity of a Range of Sulfonate Derivatives of Estrone (E1) in the Design of Reversible Inhibitors of Estrone Sulfatase (ES)

Mohsen Akbarzadeh; Timothy Cartledge; Sabbir Ahmed

Synthesis, Biological Evaluation and the Rationalisation of the Inhibitory Activity of a Range of Sulfonate Derivatives of Estrone (E1) in the Design of Reversible Inhibitors of Estrone Sulfatase (ES)

Mohsen Akbarzadeh, Timothy Cartledge, Sabbir Ahmed

University of the West of Scotland

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

Abstract

Sulfonate derivatives of estrone (E1) were designed and synthesized as potential reversible inhibitors of E1 sulfatase (ES). The results of the biochemical evaluation show the compounds to be weak inhibitors in comparison to the irreversible inhibitor E1-3-O-sulfamate, however, two compounds were found to possess good inhibitory activity.

Original language	English
Pages (from-to)	985-992
Number of pages	8
Journal	Letters in Drug Design & Discovery
Volume	11
Issue number	8
Publication status	Published - 1 Oct 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

breast cancer
estrone sulfatase
reversible inhibition
substrate mimic
sulfonated derivative

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http://www.ingentaconnect.com/content/ben/lddd/2014/00000011/00000008/art00006

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Akbarzadeh, M., Cartledge, T., & Ahmed, S. (2014). Synthesis, Biological Evaluation and the Rationalisation of the Inhibitory Activity of a Range of Sulfonate Derivatives of Estrone (E1) in the Design of Reversible Inhibitors of Estrone Sulfatase (ES). Letters in Drug Design & Discovery, 11(8), 985-992. http://www.ingentaconnect.com/content/ben/lddd/2014/00000011/00000008/art00006

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abstract = "Sulfonate derivatives of estrone (E1) were designed and synthesized as potential reversible inhibitors of E1 sulfatase (ES). The results of the biochemical evaluation show the compounds to be weak inhibitors in comparison to the irreversible inhibitor E1-3-O-sulfamate, however, two compounds were found to possess good inhibitory activity.",

keywords = "breast cancer, estrone sulfatase, reversible inhibition, substrate mimic, sulfonated derivative",

author = "Mohsen Akbarzadeh and Timothy Cartledge and Sabbir Ahmed",

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Akbarzadeh, M, Cartledge, T & Ahmed, S 2014, 'Synthesis, Biological Evaluation and the Rationalisation of the Inhibitory Activity of a Range of Sulfonate Derivatives of Estrone (E1) in the Design of Reversible Inhibitors of Estrone Sulfatase (ES)', Letters in Drug Design & Discovery, vol. 11, no. 8, pp. 985-992. <http://www.ingentaconnect.com/content/ben/lddd/2014/00000011/00000008/art00006>

Synthesis, Biological Evaluation and the Rationalisation of the Inhibitory Activity of a Range of Sulfonate Derivatives of Estrone (E1) in the Design of Reversible Inhibitors of Estrone Sulfatase (ES). / Akbarzadeh, Mohsen; Cartledge, Timothy; Ahmed, Sabbir.
In: Letters in Drug Design & Discovery, Vol. 11, No. 8, 01.10.2014, p. 985-992.

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

TY - JOUR

T1 - Synthesis, Biological Evaluation and the Rationalisation of the Inhibitory Activity of a Range of Sulfonate Derivatives of Estrone (E1) in the Design of Reversible Inhibitors of Estrone Sulfatase (ES)

AU - Akbarzadeh, Mohsen

AU - Cartledge, Timothy

AU - Ahmed, Sabbir

PY - 2014/10/1

Y1 - 2014/10/1

N2 - Sulfonate derivatives of estrone (E1) were designed and synthesized as potential reversible inhibitors of E1 sulfatase (ES). The results of the biochemical evaluation show the compounds to be weak inhibitors in comparison to the irreversible inhibitor E1-3-O-sulfamate, however, two compounds were found to possess good inhibitory activity.

AB - Sulfonate derivatives of estrone (E1) were designed and synthesized as potential reversible inhibitors of E1 sulfatase (ES). The results of the biochemical evaluation show the compounds to be weak inhibitors in comparison to the irreversible inhibitor E1-3-O-sulfamate, however, two compounds were found to possess good inhibitory activity.

KW - breast cancer

KW - estrone sulfatase

KW - reversible inhibition

KW - substrate mimic

KW - sulfonated derivative

M3 - Article

SN - 1570-1808

VL - 11

SP - 985

EP - 992

JO - Letters in Drug Design & Discovery

JF - Letters in Drug Design & Discovery

IS - 8

ER -

Synthesis, Biological Evaluation and the Rationalisation of the Inhibitory Activity of a Range of Sulfonate Derivatives of Estrone (E1) in the Design of Reversible Inhibitors of Estrone Sulfatase (ES)

Abstract

UN SDGs

Keywords

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