New phenylaminopyrimidine (PAP) anticancer lead compound with high efficacy: design, synthesis, and in vitro screening

Title
New phenylaminopyrimidine (PAP) anticancer lead compound with high efficacy: design, synthesis, and in vitro screening
Authors
무스타파한동근김인태이소하
Keywords
Phenylaminopyrimidines; Kinase inhibitor; Cancer cell-lines; Selectivity; Cancer
Issue Date
2010-07
Publisher
Bulletin of the Korean Chemical Society
Citation
VOL 31, NO 7, 1848-1858
Abstract
Phenylaminopyrimidines represent a large group of new selective anticancer agents, the majority of which exert their action through the inhibition of specific kinases. In this study, a new series of N-substituted-2-aminopyrimidines has been designed and synthesized. A selected group of the synthesized derivatives was screened at a single dose concentration of 10 μM over a panel of 60 cancer cell-lines. Compound 12e has showed great inhibitory and strong lethal effect over almost all of the 60 cell-lines and accordingly was further tested in a 5-dose testing mode to determine its IC50 values, where it showed great efficacies with intermediate potencies over the tested cell-lines. The compound was also tested over a panel of 52 kinases to explore its kinase inhibitory profile, and was found to be a selective but moderate inhibitor over FLT3 kinase.
URI
http://pubs.kist.re.kr/handle/201004/37689
ISSN
0253-2964
Appears in Collections:
KIST Publication > Article
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