Development of a chimeric c-Src kinase and HDAC inhibitor.
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ABSTRACT:
SUBMITTER: Ko KS
PROVIDER: S-EPMC3763859 | biostudies-literature | 2013 Aug
REPOSITORIES: biostudies-literature
Publications
Development of a chimeric c-Src kinase and HDAC inhibitor.
Ko Kristin S KS Steffey Michael E ME Brandvold Kristoffer R KR Soellner Matthew B MB
ACS medicinal chemistry letters 20130801 8
On the basis of synergism observed between a selective c-Src kinase inhibitor with an HDAC inhibitor, the development of the first chimeric c-Src kinase and HDAC inhibitor is described. The optimized chimeric inhibitor is shown to be a potent c-Src and HDAC inhibitor. Chimeric inhibitor <b>4</b> is further shown to be highly efficacious in cancer cell lines and significantly more efficacious than a dual-targeting strategy using discrete c-Src and HDAC inhibitors. ...[more]
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