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Andrew James Woodhead
Researcher at Astex
Publications - 34
Citations - 2152
Andrew James Woodhead is an academic researcher from Astex. The author has contributed to research in topics: Ring (chemistry) & Fragment-based lead discovery. The author has an hindex of 14, co-authored 33 publications receiving 2033 citations.
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Journal ArticleDOI
Recent Developments in Fragment-Based Drug Discovery
TL;DR: This review will look in some detail at representative protein-ligand complexes observed between fragment-sized molecules and their protein targets from the Protein Data Bank (PDB), along with the approaches that can be used to optimize fragments into lead molecules.
Journal ArticleDOI
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.
Paul Graham Wyatt,Andrew James Woodhead,Valerio Berdini,John A. Boulstridge,Maria Grazia Carr,David M. Cross,Deborah J. Davis,Lindsay A. Devine,Theresa Rachel Early,Ruth Feltell,E. Jonathan Lewis,Rachel McMenamin,Eva Figueroa Navarro,Michael Alistair O'brien,Marc O'Reilly,Matthias Reule,Gordon Saxty,Lisa C A Seavers,Donna-Michelle Smith,M. Squires,Gary Trewartha,Margaret T. Walker,Alison Jo-Anne Woolford +22 more
TL;DR: The structure-guided optimization of indazole is detailed, using information gained from multiple ligand-CDK2 cocrystal structures, which led to the identification of 33 (AT7519), which is currently being evaluated in clinical trials for the treatment of human cancers.
Journal ArticleDOI
Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design.
Andrew James Woodhead,Hayley Angove,Maria Grazia Carr,Gianni Chessari,Miles Congreve,Joseph E. Coyle,Jose Cosme,Brent Graham,Philip J. Day,Robert Downham,Lynsey Fazal,Ruth Feltell,Eva Figueroa,Martyn Frederickson,Jonathan Lewis,Rachel McMenamin,Christopher W. Murray,M. Alistair O’Brien,Lina Parra,Sahil Patel,Theresa Rachael Phillips,David C. Rees,Sharna J. Rich,Donna-Michelle Smith,Gary Trewartha,Mladen Vinkovic,Brian John Williams,Alison Jo-Anne Woolford +27 more
TL;DR: The structure guided optimization of the 2,4-dihydroxybenzamide lead molecule 1 is described and some of the drug discovery strategies employed in the identification of AT13387, which has progressed through preclinical development and is currently being tested in man.
Journal ArticleDOI
From fragment to clinical candidate--a historical perspective.
TL;DR: In this review, a historical perspective of how rapidly fragment-based drug discovery has developed is given and a number of clinical compounds discovered using this approach are described.
Journal ArticleDOI
Identification of Novel P38Alpha Map Kinase Inhibitors Using Fragment-Based Lead Generation.
Adrian Liam Gill,Martyn Frederickson,Anne Cleasby,Steven John Woodhead,Maria Grazia Carr,Andrew James Woodhead,Margaret T. Walker,Miles Congreve,Lindsay A. Devine,Dominic Tisi,Marc O'Reilly,Lisa C A Seavers,Deborah J. Davis,Jayne Curry,Rachel Anthony,Alessandro Padova,Christopher W. Murray,Robin A. E. Carr,Harren Jhoti +18 more
TL;DR: The structure-guided optimization of the molecular fragments 2-amino-3-benzyloxypyridine 1 and 3-(2-(4-pyridyl)ethyl)indole 2 identified using X-ray crystallographic screening of p38alpha MAP kinase produces two potent lead series that demonstrate significant increases in activity.