Výsledky vyhledávání - "Graham John Warrellow"

CDP840. A prototype of a novel class of orally active anti-Inflammatory phosphodiesterase 4 inhibitors

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:1451-1456

The discovery, synthesis and biological activity of a series of triarylethane phosphodiesterase 4 inhibitors is described. Structure-activity relationship studies are presented for CDP840 (29), a potent, chiral, selective inhibitor of PDE 4 (IC(50) 4

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::74d1a5dd3d9373fea6d98706204952b2
https://doi.org/10.1016/s0960-894x(02)00202-0

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Discovery and evaluation of potent, tyrosine-based α4β1 integrin antagonists

Autor: D W Howat, John Robert Porter, Neil Gozzard, Martyn Kim Robinson, W M Abraham, Graham John Warrellow, Anthony Shock, Sarah Catherine Archibald, John Clifford Head, Ted A.H. Parton

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 10:997-999

Using disulphide cysteine-based inhibitors as lead structures, this communication describes our strategy for identifying more stable, potent antagonists of the alpha4beta1 integrin. These studies ultimately discovered potent, low molecular weight inh

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3ded68239129cda0bbe1ec2b0bb8fb66
https://doi.org/10.1016/s0960-894x(00)00147-5

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Dehydrophenylalanine derivatives as VLA-4 integrin antagonists

Autor: John Robert Porter, David Critchley, Richard J. K. Taylor, Kirstie Childs, Anthony Shock, Julien Alistair Brown, Graham John Warrellow, Ted A.H. Parton, John Clifford Head, Sarah Catherine Archibald, Martyn Kim Robinson

Publikováno v: Bioorganicmedicinal chemistry letters. 13(5)

We describe a series of dehydrophenylalanine derivatives where the Z isomers are potent VLA-4 antagonists but are subject to rapid biliary clearance and the E isomers have poor activity but have a slower rate of clearance. These configurationally con

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ffdb52164735b892925f4740ea62059e
https://pubmed.ncbi.nlm.nih.gov/12617895

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Discovery and evaluation of N-(triazin-1,3,5-yl) phenylalanine derivatives as VLA-4 integrin antagonists

Autor: Alex Zomaya, John Robert Porter, Ted A.H. Parton, Brian Hutchinson, David Critchley, John Clifford Head, Kirstie Childs, Graham John Warrellow, Anthony Shock, Martyn Kim Robinson, Sarah Catherine Archibald, Julien Alistair Brown

Publikováno v: Bioorganicmedicinal chemistry letters. 12(12)

SAR studies aimed at improving the rate of clearance of a series of VLA-4 integrin antagonists by the introduction of a 1,3,5-triazine as an amide isostere are described.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::70d99b25a281d7a2443c530160b4b52c
https://pubmed.ncbi.nlm.nih.gov/12039569

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Squaric acid derivatives as VLA-4 integrin antagonists

Autor: David Critchley, John Robert Porter, Janeen Marsha Linsley, Kirstie Childs, Sarah Catherine Archibald, Rikki Peter Alexander, Ted A.H. Parton, Barry John Langham, Anthony Shock, Richard J. K. Taylor, Graham John Warrellow, Martyn Kim Robinson, John Clifford Head

Publikováno v: Bioorganicmedicinal chemistry letters. 12(7)

SAR studies aimed at improving the rate of clearance by the incorporation of a 3,4-diamino-3-cyclobutene-1,2-dione group as an amino acid isostere in a series of VLA-4 integrin antagonists are described.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c8f96d7df9023c57ef2b4c728048193
https://pubmed.ncbi.nlm.nih.gov/11909715

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Discovery and evaluation of potent, cysteine-based alpha4beta1 integrin antagonists

Autor: John Robert Porter, Anthony Shock, Martyn Kim Robinson, Janeen Marsha Linsley, Graham John Warrellow, John Clifford Head, Sarah Catherine Archibald

Publikováno v: Bioorganicmedicinal chemistry letters. 10(9)

Acyclic, disulphide derivatives of cysteine have been identified as moderately potent antagonists of α4β1-mediated leukocyte cell adhesion to VCAM. This communication describes how they were discovered from a simple l -cystine derivative and using

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c9eff5d6ee04e69524cac7b352b6c344
https://pubmed.ncbi.nlm.nih.gov/10853676

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Mechanism of Action

Autor: Graham John Warrellow, Brookings Daniel Christopher, John Robert Porter, Timothy John Norman, Rapecki Stephen Edward, Alastair D. G. Lawson, O'connell James Philip, Boris Kroeplien, David McMillan, Alexander Rikki Peter

Publikováno v: Environmental Toxin Series ISBN: 9783642705588

The invention is in the field of TNF signalling. Compounds have been identified which are capable of modulating signalling of TNF trimers through receptors. Methods of identifying such compounds are therefore provided. The compounds themselves have u

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3391dca3850192428322a5125ae15a12
https://doi.org/10.1007/978-3-642-70556-4_3

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