Polymer-assisted, multi-step solution phase synthesis and biological screening of histone deacetylase inhibitors.
The polymer-assisted solution phase synthesis (PASP) of an array of histone deacetylase (HDAc) inhibitors is described. HDAc inhibitors have considerable potential as new anti-proliferative agents. Selected compounds were shown to inhibit both human endothelial cell proliferation, and the formation of tubules (neovascularisation) in an in vitro model of angiogenesis.
Bapna
Akanksha
A
GlaxoSmithKline Cambridge Technology Centre, University Chemical Laboratory, Lensfield Road, Cambridge, UK.
Vickerstaffe
Emma
E
Warrington
Brian H
BH
Ladlow
Mark
M
Fan
Tai-Ping D
TP
Ley
Steven V
SV
D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D018920:Coculture Techniques; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D009389:Neovascularization, Pathologic / Q000473:pathology; D011108:Polymers / Q000737:chemistry*
D056572:Histone Deacetylase Inhibitors; D011108:Polymers