Abstract
We describe the synthesis of a series of low molecular weight inhibitors of the αvβ3 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.
Original language | English |
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Pages (from-to) | 657-661 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 14 |
Issue number | 3 |
DOIs | |
Publication status | Published - Feb 9 2004 |
Keywords
- αvβ3
- Angiogenesis
- Cancer
- Integrins
- Solid phase
ASJC Scopus subject areas
- Biochemistry
- Molecular Biology
- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science