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


Vol. 31,  No. 7, pp. 1848-1858, Jul.  2010
10.5012/bkcs.2010.31.7.1848


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  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 I50 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.

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  Cite this article

[IEEE Style]

I. M. E. Deeb, D. K. Han, I. T. Kim, S. H. Lee, "New Phenylaminopyrimidine (PAP) Anticancer Lead Compound with High Efficacy: Design, Synthesis, and in vitro Screening," Bulletin of the Korean Chemical Society, vol. 31, no. 7, pp. 1848-1858, 2010. DOI: 10.5012/bkcs.2010.31.7.1848.

[ACM Style]

Ibrahim Mustafa El Deeb, Dong Keun Han, In Tae Kim, and So Ha Lee. 2010. New Phenylaminopyrimidine (PAP) Anticancer Lead Compound with High Efficacy: Design, Synthesis, and in vitro Screening. Bulletin of the Korean Chemical Society, 31, 7, (2010), 1848-1858. DOI: 10.5012/bkcs.2010.31.7.1848.

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ISSN(Print) 0253-2964
ISSN(Online) 1229-5949