Výsledky vyhledávání - "Geoffrey Lawton"

Design and synthesis of the cartilage protective agent (CPA, Ro32-3555)

Autor: P.J. Malsher, Michael J. Broadhurst, K. M. K. Bottomley, Geoffrey Lawton, Brown Paul Anthony, M.I. Cooper, J. S. Nixon, Ian Reginald Kilford, Neera Borkakoti, William Henry Johnson, N. Ballantyne, A.J. Eatherton, B.M. Sutton, E. J. Lewis

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 7:2299-2302

A novel series of MMP inhibitors has been identified. The compounds are potent selective inhibitors of collagenase with good solubility and oral bioavailability. One compound, designated Ro32-3555, has been selected for development as a cartilage pro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2abba5802c7d4c274e7e5bc1f9ae53df
https://doi.org/10.1016/s0960-894x(97)00416-2

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Inhibition of bovine nasal cartilage degradation by selective matrix metalloproteinase inhibitors

Autor: Hans Werner Lahm, Pat Eyers, Brown Paul Anthony, Michael J. Broadhurst, L H Elliott, John M. Budd, Trevor J. Hallam, Urs Röthlisberger, David Bradshaw, Geoffrey Lawton, Amanda Whittle, J. S. Nixon, Maisie James, Hill Christopher Huw, Janet E. Merritt, Neera Borkakoti, William Henry Johnson, Balraj Krishnan Handa, K. M. K. Bottomley

Publikováno v: Biochemical Journal. 323:483-488

N-terminal analysis of aggrecan fragments lost from bovine nasal cartilage cultured in the presence of recombinant human interleukin 1alpha revealed a predominant ARGSVIL sequence with an additional ADLEX sequence. Production of the ARGSVIL-containin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f2481197cc0207f066b2fbffa6c53b86
https://doi.org/10.1042/bj3230483

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Bisindolylmaleimide inhibitors of protein kinase C. Further conformational restriction of a tertiary amine side chain

Autor: Sandra E. Wilkinson, Janet L. Smith, Peter D. Davis, Harris William, David R. Vesey, John S. Nixon, Geoffrey Lawton, Christopher H. Hill, Trevor J. Hallam

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 4:1303-1308

A pharmacophore model for the localisation of the cationic binding site of bisindolylmaleimide PKC inhibitors is described. This model has been used to guide selection of further conformationally restricted tertiary amine analogues, culminating in th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f5c019c3f6f3bbf635ab492fd02ea89b
https://doi.org/10.1016/s0960-894x(01)80349-8

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Inhibitors of protein kinase C. 1. 2,3-bisarylmaleimides

Autor: Peter D. Davis, Susan E. Turner, Elizabeth Keech, Geoffrey Lawton, Steven A. Hurst, John S. Nixon, Hill Christopher Huw, Sandra E. Wilkinson

Publikováno v: Journal of Medicinal Chemistry. 35:177-184

The design and synthesis of a series of novel inhibitors of protein kinase C (PKC) is described. These 2,3-bisarylmaleimides were derived from the structural lead provided by the indolocarbazoles, staurosporine and K252a. Optimum activity required th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::36544502c92fbad08ccb036e29a951d9
https://doi.org/10.1021/jm00079a024

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K252a is a potent and selective inhibitor of phosphorylase kinase

Autor: Anthony D. Sedgwick, Peter D. Davis, L H Elliott, Geoffrey Lawton, J. S. Nixon, Sandra E. Wilkinson, Hill Christopher Huw

Publikováno v: Biochemical and Biophysical Research Communications. 171:148-154

The inhibition of phosphorylase kinase by a number of protein kinase inhibitors was examined. Both K252a and staurosporine are potent inhibitors of phosphorylase kinase with IC50 values of 1.7 nM and 0.5 nM respectively. K252a shows a 300-fold select

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf0057ad08f12869bb037721e71211f0
https://doi.org/10.1016/0006-291x(90)91369-4

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Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction

Autor: Rino A. Bit, Peter D. Davis, Lucy H. Elliott, William Harris, Christopher H. Hill, Elizabeth Keech, Hari Kumar, Geoffrey Lawton, Anna Maw, John S. Nixon, David R. Vesey, Julie Wadsworth, Sandra E. Wilkinson

Publikováno v: Journal of medicinal chemistry. 36(1)

The protein kinase inhibitor staurosporine has been used to design a series of selective bisindolylmaleimide inhibitors of protein kinase C (PKC). Guided by molecular graphics, conformational restriction of the cationic side chain has led to ATP comp

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2cd943e36f82b156e0b6e9eed2e0ad02
https://pubmed.ncbi.nlm.nih.gov/8421286

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Inhibitors of protein kinase C. 2. Substituted bisindolylmaleimides with improved potency and selectivity

Autor: Elizabeth Keech, Harris William, M. K. Hari Kumar, John S. Nixon, L H Elliott, Steven A. Hurst, Sandra E. Wilkinson, Geoffrey Lawton, Hill Christopher Huw, Davis Peter David

Publikováno v: Journal of medicinal chemistry. 35(6)

A hypothetical mode of inhibition of protein kinase C (PKC) by the natural product staurosporine has been used as a basis for the design of substituted bisindolylmaleimides with improved potency over the parent compound. Structure-activity relationsh

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ae1278979c3e06f4a53fd48df9a4ed1c
https://pubmed.ncbi.nlm.nih.gov/1552513

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Synthesis of 1,2-diazetidinones (aza-β-lactams) by photochemical ring contraction

Autor: Chris Pearson, Christopher J. Moody, Geoffrey Lawton

Publikováno v: J. Chem. Soc., Perkin Trans. 1. :877-884

Irradiation of 4-diazopyrazolidine-3,5-diones (11) in the presence of alcohols, diethylamine, or water gives 1,2-diazetidinones (12) formed by photochemical Wolff rearrangement with ring contraction followed by reaction of the resulting ketene with t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::995afddc704bad3c2ac638086a102a17
https://doi.org/10.1039/p19870000877

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