Domino approach to 2-aroyltrimethoxyindoles as novel heterocyclic combretastatin A4 analogues

被引：27

作者：

Arthuis, Martin ^{[1
,2
]}

Pontikis, Renee ^{[1
,2
]}

Chabot, Guy G. ^{[3
,4
]}

Quentin, Lionel ^{[3
,4
]}

Scherman, Daniel ^{[3
,4
]}

Florent, Jean-Claude ^{[1
,2
]}

机构：

[1] Inst Curie, Ctr Rech, F-75248 Paris 05, France

[2] CNRS, UMR 176, F-75248 Paris, France

[3] Univ Paris 05, Fac Sci Pharmaceut & Biol, F-75006 Paris, France

[4] CNRS, UMR 8151, Lab Pharmacol Chim Genet & Imagerie, INSERM,U1022, F-75006 Paris, France

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 01期

关键词：

Combretastatin; Phenstatin; Aroylindole; Tubulin; Cytotoxicity; VASCULAR DISRUPTING AGENTS; BIOLOGICAL EVALUATION; TUBULIN; DERIVATIVES; SENSITIVITY; PHOSPHATE; DRUGS;

D O I：

10.1016/j.ejmech.2010.10.018

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two series of 2-aroyltrimethoxyindoles were designed to investigate the effects of the replacement of the trimethoxyphenyl ring of phenstatin with a trimethoxyindole moiety. These compounds were efficiently prepared through a domino palladium-catalyzed sequence from 2-gem-dibromovinylanilines substituted by three methoxy groups and arylboronic acids under carbon monoxide atmosphere. These novel heterocyclic combretastatin A4 analogues were evaluated for their cell growth inhibitory properties and their ability to inhibit the tubulin polymerization. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：95 / 100

页数：6

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