The Effect of Vicinal Difluorination on the Conformation and Potency of Histone Deacetylase Inhibitors
Keyword(s):
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.
2019 ◽
Vol 20
(7)
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pp. 1616
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2005 ◽
Vol 25
(5)
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pp. 1608-1619
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2020 ◽
Vol 27
(15)
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pp. 2449-2493
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