Synthesis of N-diisopropyl phosphoryl benzyltetrahydroisoquinoline, a new class of mitochondrial complexes I and III inhibitors

被引:4
作者
Andreu, I
Cabedo, N
Tormo, JR
Bermejo, A
Mello, R
Cortes, D [1 ]
机构
[1] Univ Valencia, Dept Farmacol Farmacognosia & Farmacodinamia, E-46100 Valencia, Spain
[2] Univ Valencia, Serv Cent Soporte Invest Expt, E-46100 Valencia, Spain
关键词
D O I
10.1016/S0960-894X(00)00262-6
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
The synthesis of N-(O,O-diisopropyl phosphoryl)-benzyltetrahydroisoquinoline (3) has been achieved in a 'one pot' procedure From imine (2) and diisopropyl-phosphorochloridate (1) generated in situ (POCl3 + iPrOH). Compound 3 is the first benzyltetrahydroisoquinoline derivative found to be a potent inhibitor of mitochondrial complexes I and III, and therefore it opens a new perspective with this series of compounds as they can be considered as new class of antitumor agents. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1491 / 1494
页数:4
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