PMID

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Article Title

Organization

Application of encoded library technology (ELT) to a protein-protein interaction target: discovery of a potent class of integrin lymphocyte function-associated antigen 1 (LFA-1) antagonists.

Glaxosmithkline

Arylsulfonamide pyrimidines as VLA-4 antagonists.

Elan Pharmaceuticals

Design, synthesis, and functional evaluation of leukocyte function associated antigen-1 antagonists in early and late stages of cancer development.

Ikerchem

Discovery and development of 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101)--a small molecule antagonist of leukocyte function associated antigen-1.

Cerep

Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.

TBA

Fragment-based drug discovery.

Sunesis Pharmaceuticals

Selective alpha4beta7 integrin antagonists and their potential as antiinflammatory agents.

Genentech

N-Benzoyl amino acids as LFA-1/ICAM inhibitors 1: amino acid structure-activity relationship.

Genentech

Structure-activity relationship (SAR) of thea-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists.

Sunesis Pharmaceuticals

Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists.

Sunesis Pharmaceuticals

Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).

Bristol-Myers Squibb Research And Development

Cucurbitacins, Cell Adhesion Inhibitors from Conobea scoparioides

TBA

Four new clerodane diterpenes from the leaves of Casearia guianensis which inhibit the interaction of leukocyte function antigen 1 with intercellular adhesion molecule 1.

Searle Research And Development

Structure-activity relationship of ortho- and meta-phenol based LFA-1 ICAM inhibitors.

Biogen Idec

Design and synthesis of a series of meta aniline-based LFA-1 ICAM inhibitors.

Biogen Idec

1,4-Diazepane-2,5-diones as novel inhibitors of LFA-1.

Novartis Institutes For Biomedical Research

De novo design, synthesis, and in vitro activity of LFA-1 antagonists based on a bicyclic[5.5]hydantoin scaffold.

Cerep

Amino-substituted heterocycles as isosteres of trans-cinnamides: design and synthesis of heterocyclic biaryl sulfides as potent antagonists of LFA-1/ICAM-1 binding.

Abbott Laboratories

Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-alpha]imidazol-2-one derivatives.

Boehringer Ingelheim Pharmaceuticals

Statin-derived 1,3-oxazinan-2-ones as submicromolar inhibitors of LFA-1/ICAM-1 interaction: stabilization of the metabolically labile vanillyl side chain.

Novartis Institutes For Biomedical Research

N-Benzoyl amino acids as ICAM/LFA-1 inhibitors. Part 2: structure-activity relationship of the benzoyl moiety.

Genentech

1,4-Diazepane-2-ones as novel inhibitors of LFA-1.

Novartis Institute For Biomedical Research

Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 4. Structure-activity relationship of substituents on the benzene ring of the cinnamide.

Abbott Laboratories

Discovery of potent antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 3. Amide (C-ring) structure-activity relationship and improvement of overall properties of arylthio cinnamides.

Abbott Laboratories

Discovery and SAR of diarylsulfide cyclopropylamide LFA-1/ICAM-1 interaction antagonists.

Abbott Laboratories

Novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 2. Mechanism of inhibition and structure-based improvement of pharmaceutical properties.

Abbott Laboratories

Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 1. Identification of an additional binding pocket based on an anilino diaryl sulfide lead.

Abbott Laboratories

Discovery and evaluation of potent, tyrosine-based alpha4beta1 integrin antagonists.

Celltech Chiroscience

Selective, tight-binding inhibitors of integrin alpha4beta1 that inhibit allergic airway responses.

Biogen

Novel thiazole based heterocycles as inhibitors of LFA-1/ICAM-1 mediated cell adhesion.

R. W. Johnson Pharmaceutical Research Institute