Discovery of pyrimidyl-5-hydroxamic acids as new potent histone deacetylase inhibitors.
A series of pyrimidyl-5-hydroxamic acids was prepared for evaluation as inhibitors of histone deacetylase (HDAC). Amino-2-pyrimidinyl can be used as a linker to provide HDAC inhibitors of good enzymatic potency.
Angibaud
Patrick
P
Johnson&Johnson Pharmaceutical Research&Development (J&JPRD), Medicinal Chemistry Department, campus de Maigremont BP615, 27106 Val de Reuil, France. pangibau@PRDFR.jnj.com
Arts
Janine
J
Van Emelen
Kristof
K
Poncelet
Virginie
V
Pilatte
Isabelle
I
Roux
Bruno
B
Van Brandt
Sven
S
Verdonck
Marc
M
De Winter
Hans
H
Ten Holte
Peter
P
Marien
Ann
A
Floren
Wim
W
Janssens
Boudewijn
B
Van Dun
Jacky
J
Aerts
An
A
Van Gompel
Jacky
J
Gaurrand
Sandrine
S
Queguiner
Laurence
L
Argoullon
Jean-Michel
JM
Van Hijfte
Luc
L
Freyne
Eddy
E
Janicot
Michel
M
D049109:Cell Proliferation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005260:Female; D006367:HeLa Cells; D056572:Histone Deacetylase Inhibitors; D006801:Humans; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization
D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D006877:Hydroxamic Acids; D011743:Pyrimidines