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Tropolones and Thailandepsin B as lead-like natural compounds in the development of potent and selective histone deacetylase inhibitors.

Dilipkumar PalPadum Lal
Published in: Current drug targets (2023)
It has been observed that Tropolone derivatives act as isoenzyme-selective inhibitors of proven anticancer drug targets, histone deacetylases (HDACs). Some monosubstituted tropolones show remarkable levels of selectivity for HDAC2 and strongly inhibit the growth of T-lymphocyte cell lines. And Thailandepsins have different selective inhibition profiles than FK228. They exhibit comparable inhibitory activities to FK228 against human HDAC1, HDAC2, HDAC3, HDAC6, HDAC7, and HDAC9, but less potent inhibitory activities than FK228 toward HDAC4 and HDAC8, the latter of which may be useful. Thailandepsins possess potent cytotoxic activities toward some types of cell lines.
Keyphrases
  • histone deacetylase
  • endothelial cells
  • anti inflammatory