Design and Synthesis of New Potent Anticancer Pyrazoles with High FLT3 Kinase Inhibitory Selectivity

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Title Design and Synthesis of New Potent Anticancer Pyrazoles with High FLT3 Kinase Inhibitory Selectivity
Author El-Deeb, Ibrahim Mustafa; Lee, So Ha
Journal Name Bioorganic and Medicinal Chemistry
Year Published 2010
Place of publication United Kingdom
Publisher Elsevier
Abstract A new series of 1H- and 2H-pyrazole derivatives (35 final compounds) has been designed and synthesized in this study. A selected group (13 compounds) was then tested over a panel of 60 cancer cell lines at a single dose concentration of 10 μM. At this concentration, six compounds have showed moderate to strong mean inhibitions, and were further tested at five-dose testing mode to determine their IC50 over the 60 cell lines. The IC50 values of the tested compounds indicated high potency (as for compound 10f) as well as high efficacy (as for compound 11e). Accordingly, compound 10f was then tested at a single dose concentration of 10 μM over a panel of 54 kinases to determine its kinase inhibitory profile. The compound has showed good selectivity towards FLT3 kinase, associated with a moderate potency, with an IC50 value of 1.74 μM.
Peer Reviewed Yes
Published Yes
Alternative URI http://dx.doi.org/10.1016/j.bmc.2010.04.029
Copyright Statement Copyright 2010 Elsevier. This is the author-manuscript version of this paper. Reproduced in accordance with the copyright policy of the publisher. Please refer to the journal's website for access to the definitive, published version.
Volume 18
Issue Number 11
Page from 3961
Page to 3973
ISSN 0968-0896
Date Accessioned 2011-03-18
Date Available 2011-07-19T06:25:39Z
Language en_AU
Research Centre Institute for Glycomics
Faculty Faculty of Science, Environment, Engineering and Technology
Subject Biologically Active Molecules
URI http://hdl.handle.net/10072/37837
Publication Type Journal Articles (Refereed Article)
Publication Type Code c1x

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