Ontology highlight
ABSTRACT:
SUBMITTER: Erdeljac N
PROVIDER: S-EPMC6745648 | biostudies-literature | 2019 Sep
REPOSITORIES: biostudies-literature
Erdeljac Nathalie N Bussmann Kathrin K Schöler Andrea A Hansen Finn K FK Gilmour Ryan R
ACS medicinal chemistry letters 20190719 9
A chiral, hybrid bioisostere of the CF<sub>3</sub> and Et groups (BITE) was installed in a series of vorinostat (Zolinza) analogues, and their histone deacetylase (HDAC) inhibitory behavior was studied relative to that of their nonfluorinated counterparts. Several of these compounds containing the 1,2-difluoroethylene unit showed <i>in vitro</i> potency greater than that of the clinically approved drug itself against HDAC1. This trend was found to be general with the BITE-modified HDAC inhibitor ...[more]