Synthesis of dodecaborate-conjugated cholesterols for efficient boron delivery in neutron capture therapy

被引：38

作者：

Nakamura, Hiroyuki ^{[1
]}

Ueno, Manabu

Lee, Jong-Dae

Ban, Hyun Seung

Justus, Eugen

Fan, Ping

Gabel, Detlef

机构：

[1] Gakushuin Univ, Fac Sci, Dept Chem, Tokyo 1718588, Japan

[2] Univ Bremen, Dept Chem, D-28334 Bremen, Germany

来源：

TETRAHEDRON LETTERS | 2007年 / 48卷 / 18期

基金：

日本学术振兴会;

关键词：

UNILAMELLAR LIPOSOMES; CANCER; CARBORANE; BNCT; DERIVATIVES; CHEMISTRY; AGENTS; TUMORS;

D O I：

10.1016/j.tetlet.2007.03.043

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Dodecaborate-conjugated cholesterols 3a-c were synthesized for liposomal boron delivery systems in neutron capture therapy. The current synthesis is based on the S-alkylation protocol of the cyanoethyl-protected BSH with alkyl halides. The dodecaborate-conjugated cholesterol 3a liposome, which was prepared from dimyristoylphosphatidylcholine (DMPC), cholesterol, dodecaborate-conjugated cholesterol 3a, and polyethyleneglycol-conjugated distearoylphosphatidylethanolamine (PEG-DSPE) (1:0.5:0.5:0.1), exhibited higher cytotoxicity than BSH at the same boron concentration and IC50 values of the 3a liposome and BSH toward colon 26 cells were estimated as 25 and 78 ppm of boron concentration, respectively. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：3151 / 3154

页数：4

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