在本文中,带有 6-磷酸甘露糖类似物的新糖缀合物的制备通过以下方式进行描述:(a)通过用适当的亲核试剂亲核置换来合成环状硫酸盐前体以接近碳水化合物头基;( b )通过Huisgen的环加成反应、Julia反应或超声活化下的硫醇-烯反应在6-磷酸甘露糖类似物上引入间隔基。有了所得到的化合物,金纳米粒子可以用各种碳水化合物衍生物(糖缀合物)进行功能化,然后测试血管生成活性。据观察,将糖类似物与纳米颗粒分开的间隔物的长度和柔韧性对生物反应几乎没有影响。
在本文中,带有 6-磷酸甘露糖类似物的新糖缀合物的制备通过以下方式进行描述:(a)通过用适当的亲核试剂亲核置换来合成环状硫酸盐前体以接近碳水化合物头基;( b )通过Huisgen的环加成反应、Julia反应或超声活化下的硫醇-烯反应在6-磷酸甘露糖类似物上引入间隔基。有了所得到的化合物,金纳米粒子可以用各种碳水化合物衍生物(糖缀合物)进行功能化,然后测试血管生成活性。据观察,将糖类似物与纳米颗粒分开的间隔物的长度和柔韧性对生物反应几乎没有影响。
NOVEL MANNOPYRANOSIDE DERIVATIVES WITH ANTICANCER ACTIVITY
申请人:Montero Jean-Louis
公开号:US20120269903A1
公开(公告)日:2012-10-25
The present invention relates to mannopyranoside-derived compounds and to the use thereof as medicaments, in particular in the treatment of cancer diseases, and also to the method for preparing same and to pharmaceutical compositions comprising such compounds. Medical devices surface-treated with mannopyranoside-derived compounds according to the invention also form part of the invention.
Synthesis of gold nanoparticles bearing the Thomsen–Friedenreich disaccharide: a new multivalent presentation of an important tumor antigen
作者:Sergei A. Svarovsky、Zoltan Szekely、Joseph J. Barchi
DOI:10.1016/j.tetasy.2004.12.003
日期:2005.1
Herein we describe the synthesis gold nanoshells encapsulated with up to 90 units of the Thomsen-Friedenreich (TF) tumor-associated carbohydrate antigen (TACA) disaccharide (Galbeta1-3GaINAc-alpha-O-Ser/Thr) as well as the assembly of a suitably linked designer glycopeptide as a precursor to similar multivalent presentations on gold. The TF-coated nanoparticles are highly stable, water soluble, and easily handled. Improvements in the linker technology used to attach the disaccharide to the particles led to a robust multivalent platform for the presentation of this important carbohydrate. The antigen retains all recognition characteristics while displayed on this template as shown by several in vitro assays. This area of research could lead to the development of novel therapeutic agents that inhibit protein-carbohydrate interactions. Published by Elsevier Ltd.
[EN] CARBOHYDRATE ANTIGEN-NANOPARTICLE CONJUGATES AND USES THEREOF AS ANTIMETASTATIC AGENTS IN TREATING CANCER<br/>[FR] CONJUGUES DE NANOPARTICULES-ANTIGENES CARBOHYDRATE ET UTILISATION COMME AGENTS ANTI-METASTATIQUES DANS LE TRAITEMENT DU CANCER
申请人:US GOV HEALTH & HUMAN SERV
公开号:WO2005046722A3
公开(公告)日:2005-07-21
Gold Nanoparticles Decorated with Mannose-6-phosphate Analogues
Herein, the preparation of neoglycoconjugates bearing mannose-6-phosphate analogues is described by: (a) synthesis of a cyclic sulfate precursor to access the carbohydrate head-group by nucleophilic displacement with an appropriate nucleophile; (b) introduction of spacers on the mannose-6-phosphate analogues via Huisgen’s cycloaddition, the Julia reaction, or the thiol-ene reaction under ultrasound
在本文中,带有 6-磷酸甘露糖类似物的新糖缀合物的制备通过以下方式进行描述:(a)通过用适当的亲核试剂亲核置换来合成环状硫酸盐前体以接近碳水化合物头基;( b )通过Huisgen的环加成反应、Julia反应或超声活化下的硫醇-烯反应在6-磷酸甘露糖类似物上引入间隔基。有了所得到的化合物,金纳米粒子可以用各种碳水化合物衍生物(糖缀合物)进行功能化,然后测试血管生成活性。据观察,将糖类似物与纳米颗粒分开的间隔物的长度和柔韧性对生物反应几乎没有影响。