Design and synthesis of a novel class of histone deacetylase inhibitors.
Histone deacetylase inhibitors (HDACs) have emerged as a novel class of antiproliferative agents. Utilizing structure-based design, the synthesis of a series of sulfonamide hydroxamic acids is described. Further optimization of this series by substitution of the terminal aromatic ring yielded HDAC inhibitors with good in vitro and in vivo activities.
Lavoie
R
R
Department of Medicinal Chemistry, MethylGene Inc., 7220 Frederick-Banting, Montréal, Québec, Canada H4S 2A1.
Bouchain
G
G
Frechette
S
S
Woo
S H
SH
Abou-Khalil
E
E
Leit
S
S
Fournel
M
M
Yan
P T
PT
Trachy-Bourget
M C
MC
Beaulieu
C
C
Li
Z
Z
Besterman
J
J
Delorme
D
D
D002455:Cell Division / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D056572:Histone Deacetylase Inhibitors; D006801:Humans; D066298:In Vitro Techniques; D008958:Models, Molecular
D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors