SYNTHESIS OF [D5-ETHYL]-TAMOXIFEN - A MECHANISTIC PROBE OF TAMOXIFEN INDUCED HEPATIC DNA ADDUCT FORMATION

被引：4

作者：

HORTON, MN

JARMAN, M

POTTER, GA

机构：

[1] Drug Development Section, Cancer Research Campaign Laboratory, Institute of Cancer Research, Sutton, Surrey

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1994年 / 34卷 / 08期

关键词：

D5-ETHYL]-TAMOXIFEN; TAMOXIFEN; DNA-ADDUCT; METABOLISM; KINETIC ISOTOPE EFFECT;

D O I：

10.1002/jlcr.2580340810

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Tamoxifen which incorporates a fully deuterated ethyl group, [D5-ethyl]-tamoxifen, has been synthesised in order to probe the mechanism of tamoxifen induced hepatic DNA adduct formation. The pentadeuteroethyl group was introduced into the tamoxifen structure by treatment of the ketone precursor 1-[4-(2-chloroethoxy)phenyl]-2-phenylethanone, as its sodium enolate, with [D5]-iodoethane.

引用

页码：767 / 772

页数：6

共 16 条

[1] ANTIESTROGENIC AND ANTIFERTILITY COMPOUNDS .4. 1,1,2-TRIARYLALKAN-1-OLS AND 1,1,2-TRIARYLALK-1-ENES CONTAINING BASIC ETHER GROUPS [J].