SYNTHESIS AND INVITRO EVALUATION OF BORONATED URIDINE AND GLUCOSE DERIVATIVES FOR BORON NEUTRON-CAPTURE THERAPY

被引：105

作者：

TJARKS, W ^{[1
]}

ANISUZZAMAN, AKM ^{[1
]}

LIU, L ^{[1
]}

SOLOWAY, AH ^{[1
]}

BARTH, RF ^{[1
]}

PERKINS, DJ ^{[1
]}

ADAMS, DM ^{[1
]}

机构：

[1] OHIO STATE UNIV,DEPT PATHOL,COLUMBUS,OH 43210

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 35卷 / 09期

关键词：

D O I：

10.1021/jm00087a019

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The following boron-containing nucleoside and glucose derivatives have been synthesized as potential boron delivery agents for boron neutron capture therapy (BNCT): 2'-O-(o-carboran-1-ylmethyl)uridine (4a), 3'-O-(o-carboran-1-ylmethyl) uridine (4b), sodium 7-(uridin-2'-ylmethyl)dodecahydro-7,8-dicarba-nido-undecaborate (5), 5'-O-(o-carboran-1-ylmethyl) uridine (9), and 3'-O-(o-carboran-1-ylmethyl)-D-glucose (13). In vitro cellular uptake studies were performed with F98 rat glioma cells. Following 16 h incubation, cellular boron concentrations were determined by direct current plasma atomic emission spectroscopy (DCP-AES). Boron concentrations ranged from 65 to 103-mu-g/g of cells for the neutral closo structures compared with 1.5-mu-g/g of cells for the charged nido species. Cellular uptake of sodium mercaptoundecahydro-closo-dodecaborate (BSH), the compound currently being used in Japan for the treatment of malignant brain tumors by BNCT, was 2-mu-g/g of cells.

引用

页码：1628 / 1633

页数：6

共 26 条

[1] SYNTHESIS OF A CARBORANYL NUCLEOSIDE FOR POTENTIAL USE IN NEUTRON-CAPTURE THERAPY OF CANCER [J].