Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin alphaVbeta3.
Bioorg Med Chem Lett
; 14(3): 657-61, 2004 Feb 09.
Article
in En
| MEDLINE
| ID: mdl-14741263
ABSTRACT
We describe the synthesis of a series of low molecular weight inhibitors of the alphavbeta3 integrin obtained by modifying a high-throughput screening hit with micromolar activity. A solid phase synthesis to prepare 3-phenylthio-3-nicotinyl propionic acid derivatives, exemplified by 13c, was set up. Compounds with nanomolar activity in the biochemical assay and able to efficiently inhibit cell adhesion mediated by vitronectin have been obtained.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Phenols
/
Propionates
/
Cell Adhesion
/
Integrin alphaVbeta3
/
Niacin
Limits:
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2004
Document type:
Article
Affiliation country:
Italy