Design and synthesis of new potent anticancer pyrazoles with high FLT3 kinase inhibitory selectivity

Title
Design and synthesis of new potent anticancer pyrazoles with high FLT3 kinase inhibitory selectivity
Authors
무스타파이소하
Keywords
Anticancer; Pyrazoles; FLT3; Receptor tyrosine kinase
Issue Date
2010-06
Publisher
Bioorganic & medicinal chemistry
Citation
VOL 18, NO 11, 3961-3973
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.
URI
http://pubs.kist.re.kr/handle/201004/37568
ISSN
0968-0896
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KIST Publication > Article
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