SYNTHESIS AND BIOLOGICAL-ACTIVITY OF I-125/I-127-PHENYLBORONIC ACID-DERIVATIVES

被引：5
|
作者：
KINSEY, BM [1 ]
KASSIS, AI [1 ]
机构：
[1] HARVARD UNIV,SCH MED,SHIELDS WARREN RADIAT LAB,DEPT RADIOL,BOSTON,MA 02115
来源：
NUCLEAR MEDICINE AND BIOLOGY | 1993年 / 20卷 / 01期
关键词：
D O I：
10.1016/0969-8051(93)90132-E
中图分类号：
R8 [特种医学]; R445 [影像诊断学];
学科分类号：
1002 ; 100207 ; 1009 ;
摘要：
Three iodinated phenylboronic acids have been synthesized: 4-iodophenylboronic acid (2a), 3-(4-iodobenzenesulfonamido)phenylboronic acid (5a) and 3-(5-dimethylamino-6-iodo-1-naphthalenesulfonamido)-phenylboronic acid (6a). The corresponding no-carrier-added I-125 derivatives 2b, 5b and 6b have been prepared in good yield by selective displacement of the tributylstannyl group. Compound 6b was concentrated in vitro preferentially in HT-29 human colon carcinoma cells compared to V79 Chinese hamster lung fibroblasts and showed selective retention in PaCa-2 human pancreatic cancer cells grown as solid tumor xenografts in the nude mouse.
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页码：13 / 22
页数：10
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