Daniel F Veber

Summary

Country: USA

Publications

  1. ncbi request reprint Molecular properties that influence the oral bioavailability of drug candidates
    Daniel F Veber
    Department of Medicinal Chemistry, GlaxoSmithKline, 709 Swedeland Road, P O Box 1539, King of Prussia, Pa 19406 0939, USA
    J Med Chem 45:2615-23. 2002
  2. ncbi request reprint 4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo
    Lara S Kallander
    GlaxoSmithKline Pharmaceuticals, King of Prussia, Pennsylvania 19406, USA
    J Med Chem 48:5644-7. 2005
  3. ncbi request reprint Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors
    Dennis S Yamashita
    Department of Medicinal Chemistry, GlaxoSmithKline, 1250 S Collegeville Rd, Collegeville, Pennsylvania 19426, USA
    J Med Chem 49:1597-612. 2006
  4. ncbi request reprint Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore
    Joseph P Marino
    Department of Medicinal Chemistry, Enzymology, Oncology, and Structural Biology, GlaxoSmithKline, King of Prussia, PA 19406, USA
    J Med Chem 50:3777-85. 2007
  5. ncbi request reprint Azepanone-based inhibitors of human cathepsin L
    Robert W Marquis
    Department of Medicinal Chemistry, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA
    J Med Chem 48:6870-8. 2005
  6. ncbi request reprint An azepanone-based inhibitor of human cathepsin K with improved oral bioavailability in the rat and the monkey
    Robert W Marquis
    Departments of Medicinal Chemistry, GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
    Mol Pharm 1:97-100. 2004
  7. ncbi request reprint Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor
    Katherine L Widdowson
    GlaxoSmithKline, 709 Swedeland Road, King of Prussia, Pennsylvania 19406, USA
    J Med Chem 47:1319-21. 2004

Collaborators

Detail Information

Publications7

  1. ncbi request reprint Molecular properties that influence the oral bioavailability of drug candidates
    Daniel F Veber
    Department of Medicinal Chemistry, GlaxoSmithKline, 709 Swedeland Road, P O Box 1539, King of Prussia, Pa 19406 0939, USA
    J Med Chem 45:2615-23. 2002
    ..A threshold permeation rate is a prerequisite of oral bioavailability. The rotatable bond count does not correlate with the data examined here for the in vivo clearance rate in the rat...
  2. ncbi request reprint 4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo
    Lara S Kallander
    GlaxoSmithKline Pharmaceuticals, King of Prussia, Pennsylvania 19406, USA
    J Med Chem 48:5644-7. 2005
    ..Compound 24, a potent inhibitor of cobalt-activated hMetAP2, also inhibits human and mouse endothelial cell growth. Using a mouse matrigel model, this reversible hMetAP2 inhibitor was also shown to inhibit angiogenesis in vivo...
  3. ncbi request reprint Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors
    Dennis S Yamashita
    Department of Medicinal Chemistry, GlaxoSmithKline, 1250 S Collegeville Rd, Collegeville, Pennsylvania 19426, USA
    J Med Chem 49:1597-612. 2006
    ....
  4. ncbi request reprint Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore
    Joseph P Marino
    Department of Medicinal Chemistry, Enzymology, Oncology, and Structural Biology, GlaxoSmithKline, King of Prussia, PA 19406, USA
    J Med Chem 50:3777-85. 2007
    ..Triazoles 103 and 104 also exhibited dose-dependent activity in an aortic ring tissue model of angiogenesis highlighting the potential utility of MetAP2 inhibitors as anticancer agents...
  5. ncbi request reprint Azepanone-based inhibitors of human cathepsin L
    Robert W Marquis
    Department of Medicinal Chemistry, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA
    J Med Chem 48:6870-8. 2005
    ..Optimization of cathepsin L binding by the combination of the P3 naphthylene-1-carboxamide with the P2 beta-naphthylalanine provided 15, which is a potent, selective, and competitive inhibitor of human cathepsin L with a K(i) = 0.43 nM...
  6. ncbi request reprint An azepanone-based inhibitor of human cathepsin K with improved oral bioavailability in the rat and the monkey
    Robert W Marquis
    Departments of Medicinal Chemistry, GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
    Mol Pharm 1:97-100. 2004
  7. ncbi request reprint Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor
    Katherine L Widdowson
    GlaxoSmithKline, 709 Swedeland Road, King of Prussia, Pennsylvania 19406, USA
    J Med Chem 47:1319-21. 2004
    ..This led to the identification of a potent and highly selective CXCR2 antagonist, which in addition was shown to be functionally active both in vitro against human neutrophils and in vivo in rabbit models of ear edema and neutropenia...