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Jason Witherington,
Lee Abberley,
Benjamin R Bellenie,
Rio Boatman,
Katharine Collis,
David K Dean,
Alessandra Gaiba,
N Paul King,
Nicola Shuker,
Jon G A Steadman,
Andrew K Takle,
Gareth Sanger,
Sharon Butler,
Fiona McKay,
Alison Muir,
Kim Winborn, Robert W Ward,
Tom D Heightman
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ABSTRACT: As part of an on-going lead optimisation effort, a cross screening exercise identified an aryl sulphonyl amide hit that was optimised to afford a highly potent series of ghrelin receptor agonists.
Bioorganic & medicinal chemistry letters 01/2009; 19(3):684-7. · 2.65 Impact Factor
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Jason Witherington,
Emma L Blaney,
Vincent Bordas,
Richard L Elliott,
Alessandra Gaiba,
Neil Garton,
Philip M Green,
Antoinette Naylor,
David G Smith,
David J Spalding,
Andrew K Takle, Robert W Ward
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ABSTRACT: A series of pyridone-N-benzyl-propanoic acids have been optimised to afford potent orally bioavailable VLA-4 antagonists.
Bioorganic & Medicinal Chemistry Letters 12/2006; 16(21):5538-41. · 2.55 Impact Factor
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ABSTRACT: A novel series of pyridone inhibitors has been identified through pharmacophore analysis, as potent antagonists of VLA-4.
Bioorganic & Medicinal Chemistry Letters 05/2006; 16(8):2256-9. · 2.55 Impact Factor
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ABSTRACT: A novel series of 6-aryl-pyrazolo[3,4-b]pyridines has been identified that are potent inhibitors of glycogen synthase kinase-3 (GSK-3).
Bioorganic & Medicinal Chemistry Letters 10/2003; 13(18):3055-7. · 2.55 Impact Factor
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ABSTRACT: A series of 6-heteroaryl-pyrazolo[3,4-b]pyridines has been optimised to afford potent inhibitors of Glycogen Synthase Kinase-3 (GSK-3). These analogues display excellent selectivity over the closely related Cyclin Dependent Kinase-2 (CDK-2).
Bioorganic & Medicinal Chemistry Letters 10/2003; 13(18):3059-62. · 2.55 Impact Factor
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ABSTRACT: Introduction of a nitrogen atom into the 6-position of a series of pyrazolo[3,4-b]pyridines led to a dramatic improvement in the potency of GSK-3 inhibition. Rationalisation of the binding mode suggested participation of a putative structural water molecule, which was subsequently confirmed by X-ray crystallography.
Bioorganic & Medicinal Chemistry Letters 06/2003; 13(9):1581-4. · 2.55 Impact Factor
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ABSTRACT: A novel series of pyrazolo[3,4-b]pyridines has been identified that are potent inhibitors of glycogen synthase kinase-3 (GSK-3).
Bioorganic & Medicinal Chemistry Letters 06/2003; 13(9):1577-80. · 2.55 Impact Factor