AI Article Synopsis
- - A new series of macrocyclic compounds were created to inhibit multiple targets: HDAC, FLT3, and JAK2.
- - Some of these compounds showed strong inhibition of HDAC, FLT3, and JAK2 in both lab tests and living cells.
- - In tests, these compounds were found to be particularly effective against MV4-11 cells with a FLT3 mutation and HEL cells with a JAK2 mutation.
Article Abstract
A novel series of macrocyclic compounds were designed and synthesized as multi-target inhibitors targeting HDAC, FLT3 and JAK2. Some of these compounds exhibited potent HDAC inhibition as well as FLT3 and JAK2 inhibition under both cell-free and cellular conditions. In vitro antiproliferative assay indicated that these compounds were interestingly more cytotoxic to MV4-11 cells bearing FLT3-ITD mutation and HEL cells bearing JAK2(V617F) mutation.
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| http://dx.doi.org/10.1016/j.ejmech.2015.03.034 | DOI Listing |
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