The Effect of Vicinal Difluorination on the Conformation and Potency of Histone Deacetylase Inhibitors.

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.

SUBMITTER: Ariawan AD 

PROVIDER: S-EPMC8271401 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature