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Caroline Whitworth

GlaxoSmithKline

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Publication

Featured researches published by Caroline Whitworth.

Bioorganic & Medicinal Chemistry Letters | 2009

4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors

John Liddle; Paul Bamborough; Michael David Barker; Sebastien Andre Campos; Rick P. C. Cousins; Geoffrey J. Cutler; Heather Hobbs; Duncan S. Holmes; Chris Ioannou; Geoff W. Mellor; Mary A. Morse; Jeremy John Payne; John M. Pritchard; Kathryn J. Smith; Daniel T. Tape; Caroline Whitworth; Richard A. Williamson

The synthesis and SAR of a novel series of IKK2 inhibitors are described. Modification around the hinge binding region of the 7-azaindole led to a series of potent and selective inhibitors with good cellular activity.

Bioorganic & Medicinal Chemistry Letters | 2012

4-Phenyl-7-Azaindoles as Potent, Selective and Bioavailable Ikk2 Inhibitors Demonstrating Good in Vivo Efficacy.

John Liddle; Paul Bamborough; Michael David Barker; Sebastien Andre Campos; Chun-wa Chung; Rick P. C. Cousins; Paul Faulder; Michelle L. Heathcote; Heather Hobbs; Duncan S. Holmes; Chris Ioannou; Cesar Ramirez-Molina; Mary A. Morse; Ruth R. Osborn; Jeremy John Payne; John M. Pritchard; William L. Rumsey; Daniel T. Tape; Giorgia Vicentini; Caroline Whitworth; Rick Williamson

The lead optimization of a series of potent azaindole IKK2 inhibitors is described. Optimization of the human whole blood activity and selectivity over IKK1 in parallel led to the discovery of 16, a potent and selective IKK2 inhibitor showing good efficacy in a rat model of neutrophil activation.

Journal of Medicinal Chemistry | 2007

Factor Xa Inhibitors: S1 Binding Interactions of a Series of N-{(3S)-1-[(1S)-1-Methyl-2-Morpholin-4-Yl-2-Oxoethyl]-2-Oxopyrrolidin-3-Yl}Sulfonamides.

Chuen Chan; Alan David Borthwick; David W. Brown; Cynthia L. Burns-Kurtis; Matthew Campbell; Laiq Chaudry; Chun-wa Chung; J. Nicole Hamblin; Lisa Johnstone; Henry A. Kelly; Savvas Kleanthous; Angela Patikis; Champa Patel; Anthony J. Pateman; Stefan Senger; Gita P. Shah; John R. Toomey; Nigel S. Watson; Helen E. Weston; Caroline Whitworth; and Robert J. Young; Ping Zhou

Bioorganic & Medicinal Chemistry Letters | 2006

Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors.

Nigel S. Watson; David W. Brown; Matthew Campbell; Chuen Chan; Laiq Chaudry; Rebecca Fenwick; J. Nicole Hamblin; Claudine Haslam; Henry A. Kelly; N. Paul King; Cynthia L. Kurtis; Andrew R. Leach; Gary R. Manchee; Andrew M. Mason; Charlotte Jane Mitchell; Champa Patel; Vipulkumar Kantibhai Patel; Stefan Senger; Gita P. Shah; Helen E. Weston; Caroline Whitworth; Robert J. Young

Archive | 2002

Pyrrolidin-2-one derivatives as inhibitors of factor xa

Chuen Glaxosmithkline Chan; Julie Nicole Hamblin; Henry A. Kelly; Nigel Paul King; Andrew McMurtrie GlaxoSmithKline Mason; Vipulkumar Kantibhai Patel; Stefan Senger; Gita P. Shah; Nigel S. Watson; Helen E. Weston; Caroline Whitworth; Robert J. Young

Archive | 2002

Pyrrolidine derivatives as factor Xa inhibitors

Chuen Glaxosmithkline Chan; Julie Nicole Hamblin; Henry A. Kelly; Nigel Paul King; Andrew McMurtrie GlaxoSmithKline Mason; Vipulkumar Kantibhai Patel; Stefan Senger; Gita P. Shah; Nigel S. Watson; Helen E. Weston; Caroline Whitworth; Robert J. Young

Archive | 2007

PYRROLO[2, 3-B]PYRIDIN-4-YL-BENZENESULFONAMIDE COMPOUNDS AS IKK2 INHIBITORS

Paul Bamborough; Michael David Barker; Sebastien Andre Campos; Richard Peter Charles Cousins; Paul Faulder; Heather Hobbs; Duncan S. Holmes; Michael John Johnston; John Liddle; Jeremy John Payne; John M. Pritchard; Caroline Whitworth

Archive | 2009

Pyrrolo [2, 3-b] pyridin derivatives as ikk2 inhibitors

John Liddle; Caroline Whitworth

Archive | 2008

Sulfonamide derivatives, the preparation process thereof, and pharmaceutical compositions containing the same

Chuen Chan; Julie Nicole Hamblin; Henry A. Kelly; Nigel Paul King; Andrew Mcmurtrie Mason; Vipulkumar Kantibhai Patel; Stefan Senger; Gita P. Shah; Nigel S. Watson; Helen E. Weston; Caroline Whitworth; Robert J. Young

Archive | 2007

Pyrroloä2, 3-büpyridin-4-yl-benzenesulfonamide as IKK2 inhibitors

Paul Bamborough; Michael David Barker; Sebastien Andre Campos; Richard Peter Charles Cousins; Paul Faulder; Heather Hobbs; Duncan S. Holmes; Michael John Johnston; John Liddle; Jeremy John Payne; John M. Pritchard; Caroline Whitworth

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Stefan Senger

GlaxoSmithKline

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Gita P. Shah

GlaxoSmithKline

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Helen E. Weston

GlaxoSmithKline

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Henry A. Kelly

GlaxoSmithKline

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Heather Hobbs

GlaxoSmithKline

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John Liddle

GlaxoSmithKline

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Robert J. Young

GlaxoSmithKline

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Vipulkumar Kantibhai Patel

GlaxoSmithKline

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Nigel S. Watson

University of Hertfordshire

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Duncan S. Holmes

GlaxoSmithKline

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