Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin αVβ3

Paola Vianello, Paolo Cozzi, Arturo Galvani, Maurizio Meroni, Mario Varasi, Daniele Volpi, Tiziano Bandiera

Research output: Contribution to journalArticlepeer-review

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 languageEnglish
Pages (from-to)657-661
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number3
DOIs
Publication statusPublished - Feb 9 2004

Keywords

  • αvβ3
  • Angiogenesis
  • Cancer
  • Integrins
  • Solid phase

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Fingerprint Dive into the research topics of 'Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin αVβ3'. Together they form a unique fingerprint.

Cite this