A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units.
A series of structurally novel HDAC inhibitors, in which a hetero aromatic ring connects the spacer with the hydrophobic group, has been designed and synthesized. These new inhibitors are very potent in in vitro enzymatic assays and display antiproliferation activity against two human cancer cell lines.
Dai
Yujia
Y
Cancer Research, Abbott Laboratories, Department R47J, Building AP10, 100 Abbott Park Road, Abbott Park, IL 60031, USA. yujia.dai@abbott.com
Guo
Yan
Y
Curtin
Michael L
ML
Li
Junling
J
Pease
Lori J
LJ
Guo
Jun
J
Marcotte
Patrick A
PA
Glaser
Keith B
KB
Davidsen
Steven K
SK
Michaelides
Michael R
MR
D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D056572:Histone Deacetylase Inhibitors; D006801:Humans; D006877:Hydroxamic Acids / Q000037:antagonists & inhibitors / Q000494:pharmacology; D007202:Indicators and Reagents; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D006877:Hydroxamic Acids; D007202:Indicators and Reagents