Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases

The elaboration of a novel scaffold for the inhibition of JAK2 and FAK kinases was targeted in order to provide a dual inhibitor that could target divergent pathways for tumor cell progression.

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2012-01, Vol.22 (1), p.133-137
Main Authors: Zificsak, Craig A., Gingrich, Diane E., Breslin, Henry J., Dunn, Derek D., Milkiewicz, Karen L., Theroff, Jay P., Thieu, Tho V., Underiner, Ted L., Weinberg, Linda R., Aimone, Lisa D., Albom, Mark S., Mason, Jennifer L., Saville, Lisa, Husten, Jean, Angeles, Thelma S., Finn, James P., Jan, Mahfuza, O’Kane, Teresa M., Dobrzanski, Pawel, Dorsey, Bruce D.
Format: Article
Language:English
Subjects:
Animals
antineoplastic agents
Biological and medical sciences
Cell Line, Tumor
Chemistry, Pharmaceutical - methods
cytotoxicity
Disease Progression
Drug Design
enzyme inhibition
enzyme inhibitors
FAK
Focal Adhesion Protein-Tyrosine Kinases - chemistry
Humans
Inhibitors
Inhibitory Concentration 50
JAK2
Janus Kinase 2 - chemistry
Kinase
Medical sciences
Mice
Models, Chemical
Mutation
Neoplasms - genetics
Neoplasms - pathology
non-specific protein-tyrosine kinase
Pharmacology. Drug treatments
Protein Kinase Inhibitors - chemical synthesis
Protein Kinase Inhibitors - pharmacology
Rats
Rats, Sprague-Dawley
Signal Transduction
Time Factors
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The elaboration of a novel scaffold for the inhibition of JAK2 and FAK kinases was targeted in order to provide a dual inhibitor that could target divergent pathways for tumor cell progression.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2011.11.049