K
Kenneth Wiggall
Researcher at GlaxoSmithKline
Publications - 20
Citations - 1165
Kenneth Wiggall is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Thrombopoietin & Fatty acid synthase. The author has an hindex of 16, co-authored 20 publications receiving 1116 citations.
Papers
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Journal ArticleDOI
3-(1,1-dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones, potent inhibitors of hepatitis C virus RNA-dependent RNA polymerase.
Rosanna Tedesco,Antony N. Shaw,Ramesh Bambal,Deping Chai,Nestor O. Concha,Michael G. Darcy,Dashyant Dhanak,Duke M. Fitch,Adam T. Gates,Warren W. Gerhardt,Dina L. Halegoua,Chao Han,Glenn A. Hofmann,Victor K. Johnston,Arun C. Kaura,Nannan Liu,Richard M. Keenan,Juili Lin-Goerke,Robert T. Sarisky,Kenneth Wiggall,Michael N. Zimmerman,Kevin J. Duffy +21 more
TL;DR: The structure-activity relationships (SAR) of substituents on the quinolinone ring will be focused on, culminating in the discovery of 1-(2-cyclopropylethyl)-3-(1,1-dioxo-2H-1,2,4-benzothiadiazin-3-yl)-6-fluoro-4-hydroxy-2(1H)-quinolinone (130), an inhibitor with excellent potency in biochemical
Journal ArticleDOI
New IDH1 mutant inhibitors for treatment of acute myeloid leukemia
Ujunwa C. Okoye-Okafor,Boris Bartholdy,Jessy Cartier,Enoch Gao,Beth Pietrak,Alan R. Rendina,Cynthia M. Rominger,Chad Quinn,Angela Smallwood,Kenneth Wiggall,Alexander Joseph Reif,Schmidt Stanley J,Hongwei Qi,Huizhen Zhao,Gerard Joberty,Maria Faelth-Savitski,Marcus Bantscheff,Gerard Drewes,Chaya Duraiswami,Pat Brady,Arthur Groy,Swathi Rao Narayanagari,Iléana Antony-Debré,Kelly Mitchell,Heng Rui Wang,Yun Ruei Kao,Maximilian Christopeit,Luis A. Carvajal,Laura Barreyro,Elisabeth Paietta,Hideki Makishima,Britta Will,Nestor O. Concha,Nicholas D. Adams,Benjamin Schwartz,Michael T. McCabe,Jaroslaw P. Maciejewski,Amit Verma,Ulrich Steidl +38 more
TL;DR: Crystallographic and biochemical results demonstrated that compounds of this chemical series bind to an allosteric site and lock the enzyme in a catalytically inactive conformation, thereby enabling inhibition of different clinically relevant IDH1 mutants.
Patent
Prolyl hydroxylase inhibitors
TL;DR: In this paper, the pyrimidinetrione N-substituted glycine derivatives of formula (I) are used as antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme.
Journal ArticleDOI
Hydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis.
Kevin J. Duffy,Michael G. Darcy,Evelyne Delorme,Susan B. Dillon,Daniel F. Eppley,Connie L. Erickson-Miller,Leslie Giampa,Christopher B. Hopson,Yifang Huang,Richard M. Keenan,Peter Lamb,Lynnette Leong,Nannan Liu,Stephen G. Miller,Price Alan T,Jon Rosen,Rakhi Shah,Tony Shaw,Heather Smith,Kenneth C. Stark,Shin-Shay Tian,Curtis M. Tyree,Kenneth Wiggall,Lily Zhang,Juan I. Luengo +24 more
TL;DR: Modification of the core structure and adjustment of unwanted functionality resulted in the development of (5-oxo-1,5-dihydropyrazol-4-ylidene)hydrazines which exhibited efficacies equivalent to those of TPO in several cell-based assays designed to measure thrombopoietic activity.
Journal ArticleDOI
Identification of a Pharmacophore for Thrombopoietic Activity of Small, Non-Peptidyl Molecules. 1. Discovery and Optimization of Salicylaldehyde Thiosemicarbazone Thrombopoietin Mimics
Kevin J. Duffy,Shaw Antony N,Evelyne Delorme,Susan B. Dillon,Connie L. Erickson-Miller,Leslie Giampa,Yifang Huang,Richard M. Keenan,Peter Lamb,Nannan Liu,Stephen G. Miller,Price Alan T,Jon Rosen,Heather Smith,Kenneth Wiggall,Lihua Zhang,Juan I. Luengo +16 more
TL;DR: The application of high-throughput chemistry and purification techniques allowed for the rapid elucidation of structure-activity relationships of the thiosemicarbazones.