Generation of an Ugi library of phosphate mimic-containing compounds and identification of novel dual specific phosphatase inhibitors

G Bergnes; C L Gilliam; M D Boisclair; J L Blanchard; K V Blake; D M Epstein; K Pal

doi:10.1016/s0960-894x(99)00497-7

Generation of an Ugi library of phosphate mimic-containing compounds and identification of novel dual specific phosphatase inhibitors

Bioorg Med Chem Lett. 1999 Oct 4;9(19):2849-54. doi: 10.1016/s0960-894x(99)00497-7.

Authors

G Bergnes¹, C L Gilliam, M D Boisclair, J L Blanchard, K V Blake, D M Epstein, K Pal

Affiliation

¹ Department of Medicinal Chemistry, Mitotix, Inc., Cambridge, MA 02139, USA.

PMID: 10522704
DOI: 10.1016/s0960-894x(99)00497-7

Abstract

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.

MeSH terms

Binding, Competitive
Cell Cycle
Dipeptides / chemical synthesis
Dipeptides / pharmacology
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology
Peptide Library
Phosphates / chemical synthesis*
Phosphates / pharmacology
Phosphorylation
cdc25 Phosphatases / antagonists & inhibitors*

Substances

Dipeptides
Enzyme Inhibitors
Peptide Library
Phosphates
cdc25 Phosphatases