Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors.

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Luo Y, Liu HM, Su MB, Sheng L, Zhou YB, Li J, Lu W

Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors.

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4844-6. doi: 10.1016/j.bmcl.2011.06.046. Epub 2011 Jun 17.

PubMed ID
21745740 [ View in PubMed
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Abstract

Two natural piperamides (piperlonguminine and refrofractamide A) and their derivatives were synthesized and evaluated for inhibitory activity against histone deacetylases, as well as the HCT-116 human colon cancer cell line. The preliminary structure activity relationship was discussed. Compounds featuring a hydroxamic acid moiety exhibited moderate HDAC activity and in vitro cytotoxicity.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
VorinostatHistone deacetylase 1IC 50 (nM)120N/AN/ADetails
VorinostatHistone deacetylase 3IC 50 (nM)170N/AN/ADetails
VorinostatHistone deacetylase 6IC 50 (nM)34N/AN/ADetails