Výsledky vyhledávání - "David, Cousin"

Discovery and Optimization of Potent and Orally Available CTP Synthetase Inhibitors for Use in Treatment of Diseases Driven by Aberrant Immune Cell Proliferation

Publikováno v: Journal of Medicinal Chemistry. 65:16640-16650

Herein, we report the discovery of a first-in-class chemotype 2-(alkylsulfonamido)thiazol-4-yl)acetamides that act as pan-selective inhibitors of cytidine 5'-triphosphate synthetase (CTPS1/2), critical enzymes in the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05ef9951f3a13e9255109c54a35d4764
https://doi.org/10.1021/acs.jmedchem.2c01446

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Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2

Publikováno v: Journal of medicinal chemistry. 64(16)

Aberrant activation of the mitogen-activated protein kinase pathway frequently drives tumor growth, and the ERK1/2 kinases are positioned at a key node in this pathway, making them important targets for therapeutic intervention. Recently, a number of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62d0e8543148c5c72af0eca510047c9f
https://pubmed.ncbi.nlm.nih.gov/34387469

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Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2

Publikováno v: Journal of Medicinal Chemistry. 61:4978-4992

Aberrant activation of the MAPK pathway drives cell proliferation in multiple cancers. Inhibitors of BRAF and MEK kinases are approved for the treatment of BRAF mutant melanoma, but resistance frequently emerges, often mediated by increased signaling

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f64bcd2385197c9e1b7f9532e4d26523
https://doi.org/10.1021/acs.jmedchem.8b00421

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Synthesis and growth-inhibitory activities of imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamides related to the anti-tumour drug temozolomide, with appended silicon, benzyl and heteromethyl groups at the 3-position

Autor: Christopher J. Moody, William Lewis, Magdalena B. Foreiter, Marc G. Hummersone, Richard T. Wheelhouse, Helen S. Summers, David Cousin, Tracey D. Bradshaw, Malcolm F. G. Stevens, Jihong Zhang

Publikováno v: MedChemComm. 9:545-553

A series of 3-(benzyl-substituted)-imidazo[5,1-d]-1,2,3,5-tetrazines (13) and related derivatives with 3-heteromethyl groups has been synthesised and screened for growth-inhibitory activity in vitro against two pairs of glioma cell lines with temozol

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::37dccf8e94ea21e104fc7ba2b4b0af63
https://doi.org/10.1039/c7md00554g

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Antitumor imidazo[5,1-d]-1,2,3,5-tetrazines: compounds modified at the 3-position overcome resistance in human glioblastoma cell lines

Autor: Jihong Zhang, Marc G. Hummersone, David Cousin, Mark Frigerio, Charles S. Matthews, Tracey D. Bradshaw, Malcolm F. G. Stevens

Publikováno v: MedChemComm. 7:2332-2343

Synthetic routes to 3-substituted imidazo[5,1-d]-1,2,3,5-tetrazines structurally related to temozolomide were explored. Interaction of 4-diazoimidazole-5-carboxamide with an isocyanate afforded high product yields when the isocyanate was available in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3417c9563ac20002166b3b5e835c39ca
https://doi.org/10.1039/c6md00384b

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Synthesis and growth-inhibitory activities of imidazo[5,1

Autor: David, Cousin, Marc G, Hummersone, Tracey D, Bradshaw, Jihong, Zhang, Christopher J, Moody, Magdalena B, Foreiter, Helen S, Summers, William, Lewis, Richard T, Wheelhouse, Malcolm F G, Stevens

Publikováno v: MedChemComm. 9(3)

The synthesis and biological evaluation of imidazotetrazines substituted at N-3 is described.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::731a25fcac8a5741d6beb1c8320ca201
https://pubmed.ncbi.nlm.nih.gov/30108945

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A new approach to combretastatin D2

Autor: Hendrik W. Van Den Berg, Mark Nieuwenhuyzen, John Mann, David Cousin

Publikováno v: Org. Biomol. Chem.. 4:54-62

A concise and convergent route to combretastatin D2 is described together with some preliminary biological data.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b74d531c4c2aefd332afabeba128232a
https://doi.org/10.1039/b513515j

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Experimental studies of tip-vortex formation; influence of blade-tip geometry on the vortex characteristics

Autor: Marcel Ilie, Stephen Hirst, David Cousin, Jamison Elder, Michael Morikone

Publikováno v: 49th AIAA Aerospace Sciences Meeting including the New Horizons Forum and Aerospace Exposition.

Noise generation remains a major concern in the design of modern rotorcrafts. One of the major noise sources is associated with the blade-vortex interaction (BVI) phenomenon. The present study concerns the investigation of tip vortex formation and de

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::89c1170e60b9c42b40790fad644f962e
https://doi.org/10.2514/6.2011-1253

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Antitumour imidazotetrazines. Synthesis and chemistry of 4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide (nor-temozolomide): an intermediate for the preparation of the antitumour drug temozolomide and analogues, avoiding the use of isocyanates

Autor: David Cousin, Marc G. Hummersone, Malcolm F. G. Stevens

Publikováno v: MedChemComm. 3:1419

An efficient synthesis of 4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide (nor-temozolomide) and in situ generation of the anion of nor-temozolomide from an N-3-hydroxymethyl derivative of temozolomide are reported. Alkylation of the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::26544a67eb7c16d1e46c86fc6103f1b6
https://doi.org/10.1039/c2md20251d

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