Stepwise assembly of platinum - folic acid conjugates

被引：25

作者：

Gabano, Elisabetta ^{[1
]}

Ravera, Mauro ^{[1
]}

Cassino, Claudio ^{[1
]}

Bonetti, Samuele ^{[1
]}

Palmisano, Giovanni ^{[2
]}

Osella, Domenico ^{[1
]}

机构：

[1] Univ Peimonto Orientale A Avogadro, Dipartimento Sci Ambiente & Vita, I-15100 Alessandria, Italy

[2] Univ Insubria, Dipartimento Sci Chim & Ambientali, I-22100 Como, Italy

来源：

INORGANICA CHIMICA ACTA | 2008年 / 361卷 / 05期

关键词：

folic acid; platinum complexes; drug targeting; Kaminski's reaction; coupling agents;

D O I：

10.1016/j.ica.2007.09.020

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

Folates and folate-like molecules represent a class of vectors for drug targeting and delivery. The folate receptor (FR) is overexpressed in many human cancers, therefore folate-cytotoxic drug conjugates can deliver therapeutic agents specifically to FR positive tumours. We have linked, directly through one of the carboxylate functionalities of the folic acid ( alpha or gamma), two different chelating arms for a cytotoxic platinum moiety, namely a diamine and a dicarboxylate. Five different derivatives were synthesised by multi-step procedures, purified and characterised; unfortunately, they resulted barely soluble in water, thereby precluding any biochemical and biological tests. (c) 2007 Elsevier B. V. All rights reserved.

引用

页码：1447 / 1455

页数：9

共 45 条

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