Synthesis and biochemical evaluation of a range of 4-(n-alkanesulfonate) benzyl imidazole-based compounds as inhibitors of rat testicular 17α-hydroxylase/17,20-lyase (P45017) in the treatment of hormone-dependent prostate cancer

Pallav S. Shah; Imran Shahid; Wai-Yee Lee; Caroline P. Owen; Sabbir Ahmed

Synthesis and biochemical evaluation of a range of 4-(n-alkanesulfonate) benzyl imidazole-based compounds as inhibitors of rat testicular 17α-hydroxylase/17,20-lyase (P45017) in the treatment of hormone-dependent prostate cancer

Pallav S. Shah, Imran Shahid, Wai-Yee Lee, Caroline P. Owen, Sabbir Ahmed

University of the West of Scotland

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

Abstract

17α-Hydroxylase/17,20-lyase is a target in the treatment of hormone-dependent prostate cancer. Here we report the results of a study into a range of alkanesulfonate derivatives of 4-hydroxybenzylimidazole which show the compounds to be good inhibitors with 5 [IC50=1.11μM (17α-OHase) and IC50=1.28μM (lyase)] being the most potent but weaker than ketoconazole.

Original language	English
Pages (from-to)	1000-1009
Number of pages	10
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

17α-OHase
17α-hydroxylase/17
20-lyase
Azole
Inhibitors Lyase

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S. Shah, P., Shahid, I., Lee, W.-Y., P. Owen, C., & Ahmed, S. (2014). Synthesis and biochemical evaluation of a range of 4-(n-alkanesulfonate) benzyl imidazole-based compounds as inhibitors of rat testicular 17α-hydroxylase/17,20-lyase (P45017) in the treatment of hormone-dependent prostate cancer. Letters in Drug Design & Discovery, 11(8), 1000-1009. http://www.ingentaconnect.com/content/ben/lddd/2014/00000011/00000008/art00008

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abstract = "17α-Hydroxylase/17,20-lyase is a target in the treatment of hormone-dependent prostate cancer. Here we report the results of a study into a range of alkanesulfonate derivatives of 4-hydroxybenzylimidazole which show the compounds to be good inhibitors with 5 [IC50=1.11μM (17α-OHase) and IC50=1.28μM (lyase)] being the most potent but weaker than ketoconazole.",

keywords = "17α-OHase, 17α-hydroxylase/17, 20-lyase, Azole, Inhibitors Lyase",

author = "\{S. Shah\}, Pallav and Imran Shahid and Wai-Yee Lee and \{P. Owen\}, Caroline and Sabbir Ahmed",

year = "2014",

month = oct,

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S. Shah, P, Shahid, I, Lee, W-Y, P. Owen, C & Ahmed, S 2014, 'Synthesis and biochemical evaluation of a range of 4-(n-alkanesulfonate) benzyl imidazole-based compounds as inhibitors of rat testicular 17α-hydroxylase/17,20-lyase (P45017) in the treatment of hormone-dependent prostate cancer', Letters in Drug Design & Discovery, vol. 11, no. 8, pp. 1000-1009. <http://www.ingentaconnect.com/content/ben/lddd/2014/00000011/00000008/art00008>

Synthesis and biochemical evaluation of a range of 4-(n-alkanesulfonate) benzyl imidazole-based compounds as inhibitors of rat testicular 17α-hydroxylase/17,20-lyase (P45017) in the treatment of hormone-dependent prostate cancer. / S. Shah, Pallav; Shahid, Imran; Lee, Wai-Yee et al.
In: Letters in Drug Design & Discovery, Vol. 11, No. 8, 01.10.2014, p. 1000-1009.

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

TY - JOUR

T1 - Synthesis and biochemical evaluation of a range of 4-(n-alkanesulfonate) benzyl imidazole-based compounds as inhibitors of rat testicular 17α-hydroxylase/17,20-lyase (P45017) in the treatment of hormone-dependent prostate cancer

AU - S. Shah, Pallav

AU - Shahid, Imran

AU - Lee, Wai-Yee

AU - P. Owen, Caroline

AU - Ahmed, Sabbir

PY - 2014/10/1

Y1 - 2014/10/1

N2 - 17α-Hydroxylase/17,20-lyase is a target in the treatment of hormone-dependent prostate cancer. Here we report the results of a study into a range of alkanesulfonate derivatives of 4-hydroxybenzylimidazole which show the compounds to be good inhibitors with 5 [IC50=1.11μM (17α-OHase) and IC50=1.28μM (lyase)] being the most potent but weaker than ketoconazole.

AB - 17α-Hydroxylase/17,20-lyase is a target in the treatment of hormone-dependent prostate cancer. Here we report the results of a study into a range of alkanesulfonate derivatives of 4-hydroxybenzylimidazole which show the compounds to be good inhibitors with 5 [IC50=1.11μM (17α-OHase) and IC50=1.28μM (lyase)] being the most potent but weaker than ketoconazole.

KW - 17α-OHase

KW - 17α-hydroxylase/17

KW - 20-lyase

KW - Azole

KW - Inhibitors Lyase

M3 - Article

SN - 1570-1808

VL - 11

SP - 1000

EP - 1009

JO - Letters in Drug Design & Discovery

JF - Letters in Drug Design & Discovery

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ER -