Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors

Bioorganic & Medicinal Chemistry Letters
2011.0

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.

Knowledge Graph

Similar Paper

Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors
Bioorganic & Medicinal Chemistry Letters 2011.0
Discovery, Synthesis, and Pharmacological Evaluation of Spiropiperidine Hydroxamic Acid Based Derivatives as Structurally Novel Histone Deacetylase (HDAC) Inhibitors
Journal of Medicinal Chemistry 2011.0
Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors
European Journal of Medicinal Chemistry 2016.0
Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors
Bioorganic & Medicinal Chemistry Letters 2011.0
Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity
Bioorganic & Medicinal Chemistry Letters 2010.0
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors
European Journal of Medicinal Chemistry 2009.0
Novel amide derivatives as inhibitors of histone deacetylase: Design, synthesis and SAR
European Journal of Medicinal Chemistry 2009.0
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors
Bioorganic & Medicinal Chemistry Letters 2007.0
Synthesis and Biological Evaluation of N-Hydroxyphenylacrylamides and N-Hydroxypyridin-2-ylacrylamides as Novel Histone Deacetylase Inhibitors
Journal of Medicinal Chemistry 2010.0
Design, synthesis, and preliminary bioactivity studies of substituted purine hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors
MedChemComm 2014.0