Trifluoromethyl ketones as inhibitors of histone deacetylase.
Trifluoromethyl ketones were found to be inhibitors of histone deacetylases (HDACs). Optimization of this series led to the identification of submicromolar inhibitors such as 20 that demonstrated antiproliferative effects against the HT1080 and MDA 435 cell lines.
Frey
Robin R
RR
Cancer Research, Abbott Laboratories, Abbott Park, IL 60064, USA. robin.r.frey@abbott.com
Wada
Carol K
CK
Garland
Robert B
RB
Curtin
Michael L
ML
Michaelides
Michael R
MR
Li
Junling
J
Pease
Lori J
LJ
Glaser
Keith B
KB
Marcotte
Patrick A
PA
Bouska
Jennifer J
JJ
Murphy
Shannon S
SS
Davidsen
Steven K
SK
D000107:Acetylation; D015153:Blotting, Western; D001943:Breast Neoplasms / Q000378:metabolism; D002453:Cell Cycle / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D005354:Fibrosarcoma / Q000378:metabolism; D056572:Histone Deacetylase Inhibitors; D006657:Histones / Q000378:metabolism; D006801:Humans; D006845:Hydrocarbons, Fluorinated / Q000737:chemistry / Q000494:pharmacology; D007659:Ketones / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D006657:Histones; D006845:Hydrocarbons, Fluorinated; D007659:Ketones