The effect of vicinal difluorination on the conformation and potency of histone deacetylase inhibitors

A. Daryl Ariawan, Flora Mansour, Nicole Richardson, Mohan Bhadbhade, Junming Ho, Luke Hunter*

*Corresponding author for this work

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Abstract

Histone deacetylase enzymes (HDACs) are potential targets for the treatment of cancer and other diseases, but it is challenging to design isoform-selective agents. In this work, we created new analogs of two established but non-selective HDAC inhibitors. We decorated the central linker chains of the molecules with specifically positioned fluorine atoms in order to control the molecular conformations. The fluorinated analogs were screened against a panel of 11 HDAC isoforms, and minor differences in isoform selectivity patterns were observed.
Original languageEnglish
Article number3974
Pages (from-to)1-17
Number of pages17
JournalMolecules
Volume26
Issue number13
DOIs
Publication statusPublished - 29 Jun 2021
Externally publishedYes

Bibliographical note

Copyright the Author(s) 2021. Version archived for private and non-commercial use with the permission of the author/s and according to publisher conditions. For further rights please contact the publisher.

Keywords

  • SAHA
  • Scriptaid
  • stereoselective fluorination
  • HDAC
  • Stereoselective fluorination

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