Biphenyls as potent vitronectin receptor antagonists. Part 3: Squaric acid amides.

Urbahns, Klaus; Härter, Michael; Albers, Markus; Schmidt, Delf; Stelte-Ludwig, Beatrix; Brüggemeier, Ulf; Vaupel, Andrea; Keldenich, Jörg; Lustig, Klemens; Tsujishita, Hideki; Gerdes, Christoph

Urbahns, Klaus; Härter, Michael; Albers, Markus; Schmidt, Delf; Stelte-Ludwig, Beatrix; Brüggemeier, Ulf; Vaupel, Andrea; Keldenich, Jörg; Lustig, Klemens; Tsujishita, Hideki; Gerdes, Christoph.

Affiliation

Urbahns K; Institute of Medicinal Chemistry, Bayer Healthcare AG, Bayer-Schering Pharma, 42096 Wuppertal, Germany. Klaus.Urbahns@astrazeneca.com

Bioorg Med Chem Lett ; 17(22): 6151-4, 2007 Nov 15.

Article in En | MEDLINE | ID: mdl-17910915

ABSTRACT

ABSTRACT

Vitronectin receptor (alpha(V)beta(3)) antagonists have been implicated as a possible new treatment of restenosis following balloon angioplasty. In this work we investigate a series of novel arginine mimetic scaffolds leading to new insight of the alpha(V)beta(3)/ligand interaction. Squaric acid amide 10 is a subnanomolar alpha(V)beta(3) antagonist with improved potency on human smooth muscle cell migration.

Subject(s)

Biphenyl Compounds/pharmacology; Cyclobutanes/pharmacology; Receptors, Vitronectin/antagonists & inhibitors; Sulfonamides/pharmacology; Binding Sites/drug effects; Biphenyl Compounds/chemistry; Cyclobutanes/chemistry; Humans; Ligands; Models, Molecular; Molecular Structure; Protein Structure, Tertiary; Receptors, Vitronectin/chemistry; Structure-Activity Relationship; Sulfonamides/chemistry

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Collection: 01-internacional Database: MEDLINE Main subject: Sulfonamides / Biphenyl Compounds / Receptors, Vitronectin / Cyclobutanes Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2007 Document type: Article Affiliation country: Germany

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