Daniel F Veber
- Molecular properties that influence the oral bioavailability of drug candidatesDaniel 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...
- 4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivoLara 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...
- Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitorsDennis S Yamashita
Department of Medicinal Chemistry, GlaxoSmithKline, 1250 S Collegeville Rd, Collegeville, Pennsylvania 19426, USA
J Med Chem 49:1597-612. 2006....
- Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophoreJoseph 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...
- Azepanone-based inhibitors of human cathepsin LRobert 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...
- An azepanone-based inhibitor of human cathepsin K with improved oral bioavailability in the rat and the monkeyRobert W Marquis
Departments of Medicinal Chemistry, GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
Mol Pharm 1:97-100. 2004
- Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptorKatherine 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...