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

Journal of Medicinal Chemistry

Volumn 44, Issue 18, 2001, Pages 2913-2920

  Pei, Z ^a   Xin, Z ^a   Liu, G ^a   Li, Y ^a   Reilly, E B ^a   Lubbers, N L ^a   Huth, J R ^a   Link, J T ^a   Von Geldern, T W ^a   Cox, B F ^a   Leitza, S ^a   Gao, Y ^a   Marsh, K C ^a   DeVries, P ^a   Okasinski, G F ^a  

^a ABBOTT LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

(BENZODIOXAN 6 YL)[2 TRIFLUOROMETHYL 4 [[(3 CARBOXYPYRROLIDIN 1YL)CARBONYL]ETHENYL]PHENYL]SULFIDE; CINNAMALDEHYDE; INTERCELLULAR ADHESION MOLECULE 1; LYMPHOCYTE FUNCTION ASSOCIATED ANTIGEN 1; THIOCINNAMIDE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; CELL ADHESION; HEART INFARCTION; MOLECULAR MODEL; NONHUMAN; PROTEIN INTERACTION; PROTON NUCLEAR MAGNETIC RESONANCE; RAT; STRUCTURE ACTIVITY RELATION;

AMIDES; ANIMALS; CARDIOVASCULAR AGENTS; CELL ADHESION; CELL LINE; CINNAMATES; INTERCELLULAR ADHESION MOLECULE-1; LYMPHOCYTE FUNCTION-ASSOCIATED ANTIGEN-1; MAGNETIC RESONANCE SPECTROSCOPY; MALE; MODELS, MOLECULAR; MYOCARDIAL INFARCTION; MYOCARDIUM; NIPECOTIC ACIDS; RATS; RATS, SPRAGUE-DAWLEY; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP; SULFIDES;

EID: 0035974743     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm010059w     Document Type: Article

References (34)

1. Integrin-mediated adhesion and signaling in tumorigenesis
2. Signal transduction by cell adhesion receptors
3. Leukocyte-endothelial adhesion molecules
4. The dynamic regulation of integrin adhesiveness
5. Traffic signals for lymphocyte recirculation and leukocyte emigration: The multistep paradigm
6. The role of intergrins in inflammation
7. Membrane proteins involved in phagocyte adhesion to endothelium
8. Vivo models of leukocyte migration by activation of the leukocyte adhesion molecule (LAM-1) selectin
9. Anti-adhes
10. Administration of an anti-CD-11a monoclonal antibody in recipients of kidney transplantation: A pilot study
11. Treatment of refractory rheumatoid arthritis with a monoclonal antibody to intercellular adhesion molecule 1
12. Monoclonal antibody to lymphocyte function associated antigen-1 improves graft-versus-host disease
13. A small molecule antagonist of lfa-1-mediated cell adhesion
14. Fluorenylalkanoic and benzoic acids as novel inhibitors of cell adhesion process in leukocytes
15. Novel thiazole based heterocycles as inhibitors of LFA-1/ICAM-1 mediated cell adhesion
16. Novel hydantoin derivatives useful as LFA-1 antagonists
17. Adxanthromycin: A new inhibitor of ICAM-1/LFA-1 mediated cell adhesion from streptomyces sp NA-148
18. Discovery of novel p-Arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction 1. Identification of an addition binding pocket based on an anilino diaryl sulfide lead
19. Novel p-Arylthio cinnamides as antagonists of LFA-1/ICAM-1 interaction 2. Mechanism of inhibition and structure-based SAR improvement of pharmaceutical properties
20. Crystal structure of the a domain from the subunit of integrin CR3 (CD11b/CD18)
21. 2+-complexed crystal structures
22. Conformational changes in tertiary structure near the ligand binding site of an integrin I domain
23. NMR and mutagenesis evidence for I domain allosteric site that regulate lymphocyte function-associated antigen 1 ligand binding
24. New preparation of the N-Methyl-D-Aspartate receptor antagonist, 4-(3-Phoshponopropyl)-2-piperazincarboxylic Acid (CPP)
25. New and versatile approaches to the synthesis of cpp-related competitive NMDA antagonists. Preliminary structure-activity relationships and pharmacological evaluation
26. Reduction of experimental canine myocardial reperfusion injury by a monoclonal antibody (Anti-Mol, anti-CD11b) that inhibits leukocyte adhesion
27. Antibodies against intercellular adhesion molecule I protect against myocardial ischemia-reperfusion injury in rat
28. Hydrogen peroxide induces LFA-1-Dependent neutrophil adherence to cardiac myocytes
29. Expression of intercellular adhesion molecule-1 in rat heart with ischemia/reperfusion and limitation of infarct size by treatment with antibodies against cell adhesion molecules
30. Endothelin ETA receptor antagonist reduces myocardial infarction induced by coronary artery occlusion and reperfusion in the rat
31. PCNONLiN and NONLIN84: Software for the statistical analysis of nonlinear models
32. CSTRIP-A FORTRAN computer program for obtaining initial polyexponential estimates