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Development of dichloroacetamide pyrimidines as pyruvate dehydrogenase kinase inhibitors to reduce cancer cell growth: Synthesis and biological evaluation
Zhang S.-L.2; Zhang W.2; Xiao Q.2; Yang Z.2; Hu X.2; Wei Z.1; Tam K.Y.2
2016
Source PublicationRSC Advances
ISSN20462069
Volume6Issue:82Pages:78762-78767
Abstract

Pyruvate dehydrogenases kinases (PDKs) have recently emerged as an attractive target for anticancer treatment. Herein, we report the synthesis and biological evaluation of novel PDK1 inhibitors as anticancer agents. Of the newly synthesized compounds, N-(4,6-bis(4-(2-hydroxyacetyl)piperazin-1-yl)-2-methylpyrimidin-5-yl)-2,2-dichloroacetamide (40) is found to inhibit the growth of SF188 cancer cells with an IC value of 8.21 M. Isothermal titration calorimetry (ITC) experiments reveal that compound 40 directly binds to PDK1 with a K value of 14.7 M. Compound 40 inhibits PDK1 activity by 72.5% at a concentration of 40 , meaning it could be a useful compound to explore the pharmacology of PDK1.

DOI10.1039/c6ra14060b
URLView the original
Indexed BySCI
Language英语
WOS Research AreaChemistry
WOS SubjectChemistry, Multidisciplinary
WOS IDWOS:000382539300063
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Cited Times [WOS]:4   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Affiliation1.Southern University of Science and Technology
2.Universidade de Macau
Recommended Citation
GB/T 7714
Zhang S.-L.,Zhang W.,Xiao Q.,et al. Development of dichloroacetamide pyrimidines as pyruvate dehydrogenase kinase inhibitors to reduce cancer cell growth: Synthesis and biological evaluation[J]. RSC Advances,2016,6(82):78762-78767.
APA Zhang S.-L..,Zhang W..,Xiao Q..,Yang Z..,Hu X..,...&Tam K.Y..(2016).Development of dichloroacetamide pyrimidines as pyruvate dehydrogenase kinase inhibitors to reduce cancer cell growth: Synthesis and biological evaluation.RSC Advances,6(82),78762-78767.
MLA Zhang S.-L.,et al."Development of dichloroacetamide pyrimidines as pyruvate dehydrogenase kinase inhibitors to reduce cancer cell growth: Synthesis and biological evaluation".RSC Advances 6.82(2016):78762-78767.
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