I
Indrawan James Mcalpine
Researcher at Pfizer
Publications - 48
Citations - 830
Indrawan James Mcalpine is an academic researcher from Pfizer. The author has contributed to research in topics: Catalysis & Kinase. The author has an hindex of 16, co-authored 47 publications receiving 689 citations.
Papers
More filters
Patent
3,5 disubstituted indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
TL;DR: In this paper, disubstituted indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases, are described, and pharmaceutical compositions containing them are capable of mediating CDK dependent diseases to modulate or inhibit unwanted cell proliferation.
Journal ArticleDOI
Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.
Pei-Pei Kung,Rui Eugene Yuanjin,Simon Bergqvist,Patrick Bingham,John F. Braganza,Michael R. Collins,Mei Cui,Wade Diehl,Dac M. Dinh,Connie Fan,Valeria Fantin,Hovhannes J. Gukasyan,Wenyue Hu,Buwen Huang,Kephart Susan Elizabeth,Cody Krivacic,Robert Arnold Kumpf,Gary Li,Karen A. Maegley,Indrawan James Mcalpine,Lisa Nguyen,Sacha Ninkovic,Martha A. Ornelas,Michael Ryskin,Stephanie Scales,Sutton Scott Channing,Tatlock John H,Dominique Verhelle,Fen Wang,Peter A. Wells,Martin James Wythes,Shinji Yamazaki,Brian Yip,Xiu Yu,Zehnder Luke Raymond,Wei-Guo Zhang,Robert A. Rollins,Martin Paul Edwards +37 more
TL;DR: A new enhancer of zeste homolog 2 (EZH2) inhibitor series comprising a substituted phenyl ring joined to a dimethylpyridone moiety via an amide linkage has been designed and displayed improved LipE and on-target potency in both biochemical and cellular readouts relative to compound 18.
Journal ArticleDOI
Discovery of pyrroloaminopyrazoles as novel PAK inhibitors.
Chuangxing Guo,Indrawan James Mcalpine,Zhang Junhu,Daniel D. Knighton,Kephart Susan Elizabeth,M. Catherine Johnson,Li Haitao,Djamal Bouzida,Yang Anle,Dong Liming,Marakovits Joseph T,Tikhe Jayashree Girish,Paul G. Richardson,Lisa C. Guo,Robert Steven Kania,Martin Paul Edwards,Eugenia Kraynov,James G. Christensen,Joseph Piraino,Joseph K. T. Lee,Eleanor Dagostino,Christine Del-Carmen,Ya-Li Deng,Tod Smeal,Brion W. Murray +24 more
TL;DR: The efflux of the pyrrolopyrazole series was effectively reduced by applying multiple medicinal chemistry strategies, leading to a series of PAK inhibitors that are orally active in inhibiting tumor growth in vivo.
Journal ArticleDOI
Palladium(ii)-catalyzed γ-selective hydroarylation of alkenyl carbonyl compounds with arylboronic acids
Rei Matsuura,Tanner C. Jankins,David E. Hill,Kin S. Yang,Gary M. Gallego,Shouliang Yang,Mingying He,Fen Wang,Rohan P. Marsters,Indrawan James Mcalpine,Keary M. Engle +10 more
TL;DR: A catalytic γ-selective syn-hydroarylation of alkenyl carbonyl compounds using arylboronic acids has been developed using a substrate directivity approach with a palladium(ii) catalyst.
Patent
3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
Indrawan James Mcalpine,Deal Judith G,Johnson Mary Catherine,Kephart Susan Elizabeth,Julie Park,William Romines,Tikhe Jayashree Girish +6 more
TL;DR: In this paper, 3,5 disubstituted indazole compounds with substituted nitrogen bearing 5-membered heterocycles in the 3-position were described for mediating CDK dependent diseases to modulate and/or inhibit unwanted cell proliferation.