New phenylaminopyrimidine (PAP) anticancer lead compound with high efficacy: design, synthesis, and in vitro screening
- New phenylaminopyrimidine (PAP) anticancer lead compound with high efficacy: design, synthesis, and in vitro screening
- 무스타파; 한동근; 김인태; 이소하
- Phenylaminopyrimidines; Kinase inhibitor; Cancer cell-lines; Selectivity; Cancer
- Issue Date
- Bulletin of the Korean Chemical Society
- VOL 31, NO 7, 1848-1858
- 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.
- Appears in Collections:
- KIST Publication > Article
- Files in This Item:
There are no files associated with this item.
- RIS (EndNote)
- XLS (Excel)
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.