Cyclic RGD peptides containing azabicycloalkane reverse-turn mimics

被引：19

作者：

Belvisi, L

Caporale, A

Colombo, M

Manzoni, L

Potenza, D

Scolastico, C

Castorina, M

Cati, M

Giannini, G

Pisano, C

机构：

[1] Univ Milan, Dipartimento Chim Organ & Ind, I-20133 Milan, Italy

[2] Univ Milan, CISI, I-20090 Segrate, MI, Italy

[3] CNR, Ist Sci & Tecnol Mol, I-20133 Milan, Italy

[4] Res & Dev Sigma Tau, I-00040 Pomezia, Italy

来源：

HELVETICA CHIMICA ACTA | 2002年 / 85卷 / 12期

关键词：

D O I：

10.1002/hlca.200290017

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The Fmoc-protected lactams 3 and 4 were used to prepare cyclo(Arg-Gly-Asp-lactam) 1 and cyclo(Arg-Gly-Asp-Phe-lactam) 2, which contain the Arg-Gly-Asp (RGD) recognition motif. Their solid-phase synthesis, conformational analysis, and binding to purified alpha(v)beta(3) and alpha(v)beta(5) integrins are reported. Compound 1 was found to act as an active and selective inhibitor of the alpha(v)beta(5) integrin.

引用

页码：4353 / 4368

页数：16

共 47 条

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