title: Design and synthesis of MMP inhibitors with appended fluorescent tags for imaging and visualization of matrix metalloproteinase enzymes.
abstract: We describe the synthesis, MMP-2 and 9 potency, and in vitro evaluation of a series of α-sulfone hydroxmate MMP inhibitors conjugated to a series of dyes with different absorption/emission lamina maxima's that can be used to visualize tumors.
authors.affiliation: Department of Chemistry, Mallinckrodt Pharmaceuticals, 675 McDonnell Blvd., Hazelwood, MO 63042, United States. Electronic address: john.freskos@mallinckrodt.com.
authors.forename: John N
authors.initials: JN
authors.lastname: Freskos
authors.forename: Bethel
authors.initials: B
authors.lastname: Asmelash
authors.forename: Kimberly R
authors.initials: KR
authors.lastname: Gaston
authors.forename: Amol
authors.initials: A
authors.lastname: Karwa
authors.forename: Tim A
authors.initials: TA
authors.lastname: Marzan
authors.forename: Maureen A
authors.initials: MA
authors.lastname: Nickols
authors.forename: Thomas E
authors.initials: TE
authors.lastname: Rogers
authors.forename: Tasha
authors.initials: T
authors.lastname: Schoenstein
authors.forename: Carolyn J
authors.initials: CJ
authors.lastname: Sympson
authors.forename: Bich
authors.initials: B
authors.lastname: Vu
mesh_terms: D015195:Drug Design; D005456:Fluorescent Dyes / Q000737:chemistry*; D006801:Humans; D061986:MCF-7 Cells; D020778:Matrix Metalloproteinase 2 / Q000737:chemistry / Q000378:metabolism*; D020780:Matrix Metalloproteinase 9 / Q000737:chemistry / Q000378:metabolism*; D061965:Matrix Metalloproteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D018613:Microscopy, Confocal
chemical_list: D005456:Fluorescent Dyes; D061965:Matrix Metalloproteinase Inhibitors; D020778:Matrix Metalloproteinase 2; D020780:Matrix Metalloproteinase 9
keywords: Imaging agents; MMP inhibitors; Tumor visualazation