Design and synthesis of beta-amino-alpha-hydroxy amide derivatives as inhibitors of MetAP2 and HUVEC growth

Martin Sendzik; James W Janc; Ronnel Cabuslay; Lee Honigberg; Richard L Mackman; Catherine Magill; Neil Squires; Nancy Waldeck

doi:10.1016/j.bmcl.2004.04.004

Design and synthesis of beta-amino-alpha-hydroxy amide derivatives as inhibitors of MetAP2 and HUVEC growth

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3181-4. doi: 10.1016/j.bmcl.2004.04.004.

Authors

Martin Sendzik¹, James W Janc, Ronnel Cabuslay, Lee Honigberg, Richard L Mackman, Catherine Magill, Neil Squires, Nancy Waldeck

Affiliation

¹ Departments of Medicinal Chemistry and Biology, Celera, 180 Kimball Way, South San Francisco, CA 94080, USA. martin.sendzik@celera.com

PMID: 15149671
DOI: 10.1016/j.bmcl.2004.04.004

Abstract

The rational design and synthesis of beta-amino-alpha-hydroxy amide derivatives as reversible inhibitors of methionine aminopeptidase-2 (MetAP2) with anti-proliferative activity against human umbilical vein endothelial cells (HUVECs) is described.

MeSH terms

Amides / chemical synthesis*
Amides / pharmacology
Aminopeptidases / antagonists & inhibitors*
Aminopeptidases / metabolism
Animals
Cattle
Drug Design*
Endothelium, Vascular / drug effects*
Endothelium, Vascular / enzymology*
Glycoproteins / antagonists & inhibitors*
Glycoproteins / metabolism
Humans
Methionyl Aminopeptidases
Protease Inhibitors / chemical synthesis*
Protease Inhibitors / pharmacology

Substances

Amides
Glycoproteins
Protease Inhibitors
Aminopeptidases
METAP2 protein, human
Methionyl Aminopeptidases