Synthesis and biological activity of new melatonin dimeric derivatives

被引：44

作者：

Di Giacomo, Barbara ^{[1
]}

Bedini, Annalida

Spadoni, Gilberto

Tarzia, Giorgio

Fraschini, Franco

Pannacci, Marilou

Lucini, Valeria

机构：

[1] Univ Urbino, Inst Chim Pharmaceut, I-61029 Urbino, Italy

[2] Univ Milan, Dept Pharmacol Chemotherapy & Med Toxicol, I-20129 Milan, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 13期

关键词：

melatonin; MLT receptors; biligands; melatonin dimers;

D O I：

10.1016/j.bmc.2007.03.080

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A new series of melatonin (MLT) dimers were obtained by linking together two melatonin units with a linear alkyl chain through the MLT acetamido group or through a C-2 carboxyalkyl function. The binding properties of these ligands were evaluated in in vivo experiments on cloned human MT1 and MT2 receptors expressed in NIH3T3 rat fibroblast cells. The class of 2-carboxyalkyl dimers was the most interesting one with compounds having good MT1/MT2 nanomolar affinity. The data obtained suggest that the spacer length is crucial for optimal interaction at both receptor subtypes as well as to determine functional activity of the resulting dimers. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：4643 / 4650

页数：8

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