Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin alphaVbeta3 |
| |
Authors: | Vianello Paola Cozzi Paolo Galvani Arturo Meroni Maurizio Varasi Mario Volpi Daniele Bandiera Tiziano |
| |
Institution: | Department of Chemistry, Pharmacia Italia SpA-Gruppo Pfizer, Discovery Research Oncology, Viale Pasteur 10, 20014 (MI), Nerviano, Italy. paola.vianello@pharmacia.com |
| |
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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|