Synthesis and preliminary biological assessments of a new class of amphiphilic telomers bearing 5-fluorouracil moieties

被引：0

作者：

Contino, C

Maurizis, JC

Pucci, B

机构：

[1] Univ Avignon, Lab Chim Bioorgan & Syst Mol Vectoriels, F-84000 Avignon, France

[2] INSERM, U71, F-63005 Clermont Ferrand, France

来源：

MACROMOLECULAR CHEMISTRY AND PHYSICS | 1999年 / 200卷 / 06期

关键词：

D O I：

10.1002/(SICI)1521-3935(19990601)200:6<1351::AID-MACP1351>3.0.CO;2-O

中图分类号：

O63 [高分子化学（高聚物）];

学科分类号：

070305 ; 080501 ; 081704 ;

摘要：

The synthesis and biological studies of cotelomers derived from tris(hydroxymethyl)acrylamidomethane (THAM) and bearing 5-FU moieties are reported. These macromolecular carriers were obtained by radical cotelomerization of THAM and an N-1-acyloxymethyl derivative of 5-FU. Different telomers were prepared in order to specify the influence of the prodrug on the efficiency of the therapeutic agent. An evaluation of their cytotoxic activity was performed in vitro on a melanoma cell line B16 using the colony-forming method. It appears from these biological assays that, while the monomeric substrates are less active than free 5-FU, the multiplication of active ligands obtained by telomerization involves a sharp enhancement of the antitumoral activity.

引用

页码：1351 / 1355

页数：5

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