New Phenylaminopyrimidine (PAP) Anticancer Lead Compound with High Efficacy: Design, Synthesis, and in vitro Screening

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Title New Phenylaminopyrimidine (PAP) Anticancer Lead Compound with High Efficacy: Design, Synthesis, and in vitro Screening
Author El-Deeb, Ibrahim Mustafa; Han, Dong Keun; Kim, In Tae; Lee, So Ha
Journal Name Bulletin of the Korean Chemical Society
Year Published 2010
Place of publication South Korea
Publisher Korean Chemical Society
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.
Peer Reviewed Yes
Published Yes
Alternative URI http://dx.doi.org/10.5012/bkcs.2010.31.7.1848
Volume 31
Issue Number 7
Page from 1848
Page to 1858
ISSN 0253-2964
Date Accessioned 2011-03-18
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/10072/39884
Publication Type Journal Articles (Refereed Article)
Publication Type Code c1x

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