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

doi:10.1016/j.bmcl.2003.11.045

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

Istituto Europeo di Oncologia

Research output: Contribution to journal › Article › peer-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 language	English
Pages (from-to)	657-661
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	3
DOIs	https://doi.org/10.1016/j.bmcl.2003.11.045
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

Access to Document

10.1016/j.bmcl.2003.11.045

Cite this

Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin αVβ3. / Vianello, Paola; Cozzi, Paolo; Galvani, Arturo; Meroni, Maurizio; Varasi, Mario; Volpi, Daniele; Bandiera, Tiziano.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 14, No. 3, 09.02.2004, p. 657-661.

Research output: Contribution to journal › Article › peer-review

@article{c5fe8008fb7b44858361ff477a013aa9,

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

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.",

keywords = "αvβ3, Angiogenesis, Cancer, Integrins, Solid phase",

author = "Paola Vianello and Paolo Cozzi and Arturo Galvani and Maurizio Meroni and Mario Varasi and Daniele Volpi and Tiziano Bandiera",

year = "2004",

month = feb,

day = "9",

doi = "10.1016/j.bmcl.2003.11.045",

language = "English",

volume = "14",

pages = "657--661",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

number = "3",

}

TY - JOUR

T1 - Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin αVβ3

AU - Vianello, Paola

AU - Cozzi, Paolo

AU - Galvani, Arturo

AU - Meroni, Maurizio

AU - Varasi, Mario

AU - Volpi, Daniele

AU - Bandiera, Tiziano

PY - 2004/2/9

Y1 - 2004/2/9

N2 - 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.

AB - 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.

KW - αvβ3

KW - Angiogenesis

KW - Cancer

KW - Integrins

KW - Solid phase

UR - http://www.scopus.com/inward/record.url?scp=1642493647&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=1642493647&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2003.11.045

DO - 10.1016/j.bmcl.2003.11.045

M3 - Article

C2 - 14741263

AN - SCOPUS:1642493647

VL - 14

SP - 657

EP - 661

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 3

ER -

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

Abstract

Keywords

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this