title: Design and synthesis of beta-amino-alpha-hydroxy amide derivatives as inhibitors of MetAP2 and HUVEC growth.
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.
authors.affiliation: Departments of Medicinal Chemistry and Biology, Celera, 180 Kimball Way, South San Francisco, CA 94080, USA. martin.sendzik@celera.com
authors.forename: Martin
authors.initials: M
authors.lastname: Sendzik
authors.forename: James W
authors.initials: JW
authors.lastname: Janc
authors.forename: Ronnel
authors.initials: R
authors.lastname: Cabuslay
authors.forename: Lee
authors.initials: L
authors.lastname: Honigberg
authors.forename: Richard L
authors.initials: RL
authors.lastname: Mackman
authors.forename: Catherine
authors.initials: C
authors.lastname: Magill
authors.forename: Neil
authors.initials: N
authors.lastname: Squires
authors.forename: Nancy
authors.initials: N
authors.lastname: Waldeck
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology; D000626:Aminopeptidases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D002417:Cattle; D015195:Drug Design; D004730:Endothelium, Vascular / Q000187:drug effects* / Q000201:enzymology*; D006023:Glycoproteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D063208:Methionyl Aminopeptidases; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000577:Amides; D006023:Glycoproteins; D011480:Protease Inhibitors; D000626:Aminopeptidases; C081311:METAP2 protein, human; D063208:Methionyl Aminopeptidases