The Effect of Vicinal Difluorination on the Conformation and Potency of Histone Deacetylase Inhibitors.
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ABSTRACT:
SUBMITTER: Ariawan AD
PROVIDER: S-EPMC8271401 | biostudies-literature | 2021 Jun
REPOSITORIES: biostudies-literature
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The Effect of Vicinal Difluorination on the Conformation and Potency of Histone Deacetylase Inhibitors.
Ariawan A Daryl AD Mansour Flora F Richardson Nicole N Bhadbhade Mohan M Ho Junming J Hunter Luke L
Molecules (Basel, Switzerland) 20210629 13
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 ...[more]
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