Synthesis of cotelomers derived from tris(hydroxymethyl)acrylamidomethane (THAM) bearing cytosine arabinoside moieties. Preliminary investigation of their biological activity.

被引:8
作者
Contino, C
Ollier, M
Maurizis, JC
Lacombe, JM
Pucci, B
机构
[1] UNIV AVIGNON,LAB CHIM BIOORGAN & SYST MOL VECTORIELS,F-84000 AVIGNON,FRANCE
[2] UNITE INSERM U71,F-63005 CLERMONT FERRAN,FRANCE
关键词
D O I
10.1016/S0040-4039(96)02122-3
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The telomerization of tris(hydroxymethyl)acrylamidomethane (THAM) and cytosine arabinoside (Ara-C) polymerizable derivatives in the presence of transfer reagent such as alkane or perfluoroalkane thiol is described. The cytotoxic activities of these different compounds are determined on B16, a mouse melanoma cell line. Noteworthy is that all telomers exhibit a biological activity. These preliminary results show that macromolecular carriers such as cotelomers penetrate into the cell and release the drug after an enzymatic hydrolysis. Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码:9049 / 9052
页数:4
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