Generation of an Ugi library of phosphate mimic-containing compounds and identification of novel dual specific phosphatase inhibitors.
The four-component Ugi reaction was utilized to prepare a library of dipeptidic compounds in order to explore the binding requirements of the key cell cycle phosphatase, Cdc25. Several phosphate surrogates were incorporated into the Ugi product to mimic either the mono- or bis-phosphorylated substrate.
Bergnes
G
G
Department of Medicinal Chemistry, Mitotix, Inc., Cambridge, MA 02139, USA.
Gilliam
C L
CL
Boisclair
M D
MD
Blanchard
J L
JL
Blake
K V
KV
Epstein
D M
DM
Pal
K
K
D001667:Binding, Competitive; D002453:Cell Cycle; D004151:Dipeptides / Q000138:chemical synthesis / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D019151:Peptide Library; D010710:Phosphates / Q000138:chemical synthesis* / Q000494:pharmacology; D010766:Phosphorylation; D020687:cdc25 Phosphatases / Q000037:antagonists & inhibitors*
D004151:Dipeptides; D004791:Enzyme Inhibitors; D019151:Peptide Library; D010710:Phosphates; D020687:cdc25 Phosphatases