Inhibition of tumor necrosis factor-α (TNF-α) production and arthritis in the rat by GW3333, a dual inhibitor of TNF-α-converting enzyme and matrix metalloproteinases

…, RC Crumrine, MA Leenitzer, DL McDougald… - … of Pharmacology and …, 2001 - ASPET
Tumor necrosis factor-α (TNF)-converting enzyme (TACE) cleaves the precursor form of TNF,
allowing the mature form to be secreted into the extracellular space. GW3333, a dual …

Design of selective and soluble inhibitors of tumor necrosis factor-α converting enzyme (TACE)

…, MA Leesnitzer, DL McDougald… - Journal of Medicinal …, 2001 - ACS Publications
A program to improve upon the in vitro, in vivo, and physicochemical properties of N-hydroxyformamide
TACE inhibitor GW 3333 (1) is described. Using the primary structure of pro-TNF-…

Structure-based design of potent retinoid X receptor α agonists

…, JM Lenhard, AB Miller, DL McDougald… - Journal of medicinal …, 2004 - ACS Publications
A series of tetrahydrobenzofuranyl and tetrahydrobenzothienyl propenoic acids that showed
potent agonist activity against RXRα were synthesized via a structure-based design …

Convergent catalytic asymmetric synthesis of camptothecin analog GI147211C

…, GC Lewis, TC Lovelace, MW Lowery, DL McDougald… - Tetrahedron, 1997 - Elsevier
The topoisomerase I inhibitor GI147211C (4) was discovered at Glaxo Wellcome and shown
to have promising anti-cancer properties. In order to fully assess the clinical potential of 4, …

Synthesis and pharmacological characterization of 1-phenyl-, 4-phenyl-, and 1-benzyl-1, 2, 3, 4-tetrahydroisoquinolines as dopamine receptor ligands

…, JP Bowen, DL McDougald… - Journal of medicinal …, 1988 - ACS Publications
A series of 1-phenyl-, 4-phenyl-, and 1-benzyl-l, 2, 3, 4-tetrahydroisoquinolines have been
prepared as ring-contracted analogues of the prototypical Dj dopamine receptor antagonist …

2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV

CD Haffner, DL McDougald, SM Reister… - Bioorganic & medicinal …, 2005 - Elsevier
We report the synthesis and biological activity of a series of 2-cyano-4-fluoro-1-thiovalylpyrrolidine
inhibitors of DPP-IV. Within this series, compound 19 provided a potent, selective, and …

Substrate specificity and novel selective inhibitors of TNF-α converting enzyme (TACE) from two-dimensional substrate mapping

…, JD Becherer, DL McDougald… - … chemistry & high …, 2005 - ingentaconnect.com
We report a systematic analysis of the P1' and P2' substrate specificity of TNF-α converting
enzyme (TACE) using a peptide library and a novel analytical method, and we use the …

Targeting aldehyde dehydrogenase: a potential approach for cell labeling

…, H Song, D Affleck, DL McDougald… - Nuclear medicine and …, 2009 - Elsevier
INTRODUCTION: To advance the science and clinical application of stem cell therapy, the
availability of a highly sensitive, quantitative and translational method for tracking stem cells …

N-Hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1′ isobutyl substitution

…, MH Lambert, MA Leesnitzer, DL McDougald… - Bioorganic & medicinal …, 2001 - Elsevier
N-Hydroxyformamide-class metalloprotease inhibitors were designed and synthesized, which
have potent broad-spectrum activity versus matrix metalloproteases and TNF-α converting …

Multiple tritium labelling of (+)‐7‐chloro‐8‐hydroxy‐1‐phenyl‐3‐methyl‐2,3,4,5‐tetrahydro‐1hZ‐3‐benzazepine (sch23390)

SD Wyrick, DL McDougald… - Journal of Labelled …, 1986 - Wiley Online Library
We previously reported the synthesis of the antidopaminergic‐antipsychotic agent SCH23390
labelled with tritium In the 9 position of the benzazepine ring system at a specific activity of …