J
John S. Tokarski
Researcher at Bristol-Myers Squibb
Publications - 70
Citations - 4936
John S. Tokarski is an academic researcher from Bristol-Myers Squibb. The author has contributed to research in topics: Kinase & Tyrosine kinase. The author has an hindex of 30, co-authored 65 publications receiving 4557 citations. Previous affiliations of John S. Tokarski include Princeton University.
Papers
More filters
Journal ArticleDOI
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
Louis J. Lombardo,Francis Y. Lee,Ping Chen,Derek J. Norris,Joel C. Barrish,Kamelia Behnia,Stephen Castaneda,Cornelius Lyndon A M,Jagabandhu Das,Arthur M. Doweyko,Craig Fairchild,John T. Hunt,Ivan Inigo,Kathy A. Johnston,Amrita Kamath,David Kan,Herbert E. Klei,Punit Marathe,Suhong Pang,Russell Peterson,Sidney Pitt,Gary L. Schieven,Robert J. Schmidt,John S. Tokarski,Mei-Li Wen,John Wityak,Robert M. Borzilleri +26 more
TL;DR: Compound 13 was orally active in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels.
Journal ArticleDOI
The Structure of Dasatinib (BMS-354825) Bound to Activated ABL Kinase Domain Elucidates Its Inhibitory Activity against Imatinib-Resistant ABL Mutants
John S. Tokarski,John A. Newitt,Chieh Ying J. Chang,Janet D. Cheng,Michael Wittekind,Susan E. Kiefer,Kevin Kish,Francis Y.F. Lee,Robert Borzillerri,Louis J. Lombardo,Dianlin Xie,Yaqun Zhang,Herbert E. Klei +12 more
TL;DR: Analysis of the crystal structure of dasatinib-bound ABL kinase suggests that the increased binding affinity of d asatinib over imatinib is at least partially due to its ability to recognize multiple states of BCR-ABL.
Journal ArticleDOI
Discovery of N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily
Gretchen M. Schroeder,Yongmi An,Zhen-Wei Cai,Xiao-Tao Chen,Cheryl M. Clark,Cornelius Lyndon A M,Jun Dai,Johnni Gullo-Brown,Ashok Kumar Gupta,Benjamin J. Henley,John T. Hunt,Robert Jeyaseelan,Amrita Kamath,Kyoung S. Kim,Jonathan Lippy,Louis J. Lombardo,Veeraswamy Manne,Simone Oppenheimer,John S. Sack,Robert J. Schmidt,Guoxiang Shen,Kevin Stefanski,John S. Tokarski,George L. Trainor,Barri Wautlet,Donna D. Wei,David K. Williams,Yingru Zhang,Yueping Zhang,Joseph Fargnoli,Robert M. Borzilleri +30 more
TL;DR: Analogue 10 demonstrated complete tumor stasis in a Met-dependent GTL-16 human gastric carcinoma xenograft model following oral administration and has been advanced into phase I clinical trials.
Journal ArticleDOI
N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.
Raj N. Misra,Hai-Yun Xiao,Kyoung S. Kim,Songfeng Lu,Wen-Ching Han,Stephanie Barbosa,John T. Hunt,Rawlins David B,Weifang Shan,Syed Z. Ahmed,Ligang Qian,Bang-Chi Chen,Rulin Zhao,Mark S. Bednarz,Kristen A. Kellar,Janet G. Mulheron,Roberta Batorsky,Urvashi V. Roongta,Amrita Kamath,Punit Marathe,Sunanda A. Ranadive,John S. Sack,John S. Tokarski,Nikola P. Pavletich,Francis Y. Lee,Kevin R. Webster,S. David Kimball +26 more
TL;DR: Ncyl-2-aminothiazoles with nonaromatic acyl side chains containing a basic amine were found to be potent, selective inhibitors of CDK2/cycE which exhibit antitumor activity in mice.
Patent
Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases
Bang-Chi Chen,Ping Chen,John Hynes,Peter A. Kiener,Katerina Leftheris,Malinda Longphre,Derek J. Norris,Chennagiri R. Pandit,Steven H. Spergel,John S. Tokarski,Stephen T. Wrobleski,Hong Wu,Rulin Zhao +12 more
TL;DR: In this paper, the use of a compound for treating a respiratory disease in a mammal wherein the compound is a cannabinoid receptor modulator is disclosed, and compounds useful as CBR modulators for treating respiratory and non-respiratory leukocyte activation associated diseases comprise compounds of formula (I), in which A and B are nitrogen or carbon, provided only one of a and B is nitrogen; and R1-R6 are as defined in the specification, wherein R2 with R5 may form a ring, and/or two R4 groups may form six-membered a