The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist

Joseph Rimland; Angela Dunne; Suchete S Hunjan; Rosemary Sasse; Iain Uings; Dino Montanari; Matilde Caivano; Poonam Shah; David Standing; David Gray; David Brown; William Cairns; Ryan Trump; Paul W Smith; Nicolas Bertheleme; Pier D'Alessandro; Sheraz Gul; Mythily Vimal; David N Smith; Stephen P Watson

doi:10.1016/j.bmcl.2010.01.133

The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist

Joseph Rimland
, Angela Dunne
, Suchete S Hunjan
, Rosemary Sasse
, Iain Uings
, Dino Montanari
, Matilde Caivano
, Poonam Shah
, David Standing
, David Gray
, David Brown
, William Cairns
, Ryan Trump
, Paul W Smith
, Nicolas Bertheleme
, Pier D'Alessandro
, Sheraz Gul
, Mythily Vimal
, David N Smith
, Stephen P Watson

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

13 Citations (Scopus)

Abstract

The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A selective over PR is described. Associated structure-activity relationships and the process of optimisation of an initial HTS hit are also described.

Original language	English
Pages (from-to)	2340-3
Number of pages	4
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	20
Issue number	7
DOIs	https://doi.org/10.1016/j.bmcl.2010.01.133
Publication status	Published - Apr 2010

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10.1016/j.bmcl.2010.01.133

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Rimland, J., Dunne, A., Hunjan, S. S., Sasse, R., Uings, I., Montanari, D., Caivano, M., Shah, P., Standing, D., Gray, D., Brown, D., Cairns, W., Trump, R., Smith, P. W., Bertheleme, N., D'Alessandro, P., Gul, S., Vimal, M., Smith, D. N., & Watson, S. P. (2010). The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist. Bioorganic & Medicinal Chemistry Letters, 20(7), 2340-3. https://doi.org/10.1016/j.bmcl.2010.01.133

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abstract = "The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A selective over PR is described. Associated structure-activity relationships and the process of optimisation of an initial HTS hit are also described.",

author = "Joseph Rimland and Angela Dunne and Hunjan, \{Suchete S\} and Rosemary Sasse and Iain Uings and Dino Montanari and Matilde Caivano and Poonam Shah and David Standing and David Gray and David Brown and William Cairns and Ryan Trump and Smith, \{Paul W\} and Nicolas Bertheleme and Pier D'Alessandro and Sheraz Gul and Mythily Vimal and Smith, \{David N\} and Watson, \{Stephen P\}",

year = "2010",

month = apr,

doi = "10.1016/j.bmcl.2010.01.133",

language = "English",

volume = "20",

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journal = "Bioorganic \& Medicinal Chemistry Letters",

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Rimland, J, Dunne, A, Hunjan, SS, Sasse, R, Uings, I, Montanari, D, Caivano, M, Shah, P, Standing, D, Gray, D, Brown, D, Cairns, W, Trump, R, Smith, PW, Bertheleme, N, D'Alessandro, P, Gul, S, Vimal, M, Smith, DN & Watson, SP 2010, 'The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist', Bioorganic & Medicinal Chemistry Letters, vol. 20, no. 7, pp. 2340-3. https://doi.org/10.1016/j.bmcl.2010.01.133

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T1 - The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist

AU - Rimland, Joseph

AU - Dunne, Angela

AU - Hunjan, Suchete S

AU - Sasse, Rosemary

AU - Uings, Iain

AU - Montanari, Dino

AU - Caivano, Matilde

AU - Shah, Poonam

AU - Standing, David

AU - Gray, David

AU - Brown, David

AU - Cairns, William

AU - Trump, Ryan

AU - Smith, Paul W

AU - Bertheleme, Nicolas

AU - D'Alessandro, Pier

AU - Gul, Sheraz

AU - Vimal, Mythily

AU - Smith, David N

AU - Watson, Stephen P

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AB - The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A selective over PR is described. Associated structure-activity relationships and the process of optimisation of an initial HTS hit are also described.

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DO - 10.1016/j.bmcl.2010.01.133

M3 - Article

C2 - 20202837

SN - 1464-3405

VL - 20

SP - 2340

EP - 2343

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 7

ER -

The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist

Abstract

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