Exploring the effect of 2,3,4-trimethoxy-phenyl moiety as a component of indolephenstatins

被引：36

作者：

Alvarez, Concepcion

Alvarez, Raquel

Corchete, Purificacion ^{[2
]}

Perez-Melero, Concepcion

Pelaez, Rafael ^{[1
]}

Medarde, Manuel

机构：

[1] Univ Salamanca, Lab Quim Organ & Farmaceut, Fac Farm, Dept Quim Farmacuet, E-37007 Salamanca, Spain

[2] Univ Salamanca, Dept Fisiol Vegetal, Fac Farm, E-37007 Salamanca, Spain

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 02期

关键词：

Phenstatin; Indole; Tubulin; Combretastatin; Cytotoxicity; Antitumour; Oxime; Hydrazone; Hydrazide; Acetylderivatives; 2,3,4-Trimethoxyphenyl; POTENT ANTITUBULIN AGENTS; COMBRETASTATIN A-4 ANALOGS; CELL GROWTH INHIBITOR; SITU CROSS-DOCKING; BIOLOGICAL EVALUATION; TUBULIN POLYMERIZATION; ANTIMITOTIC AGENTS; ANTINEOPLASTIC AGENTS; DERIVATIVES; COLCHICINE;

D O I：

10.1016/j.ejmech.2009.10.047

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new family of phenstatin analogues has been synthesized and assayed. This family simultaneously incorporates modifications of the A-ring (replacement of the 3,4,5-trimethoxyphenyl by the 2,3,4-trimethoxyphenyl arrangement), B-ring (N-alkyl-5-indolyl) and conversion of the Oxygen keto group into a substituted nitrogen (oximes, hydrazones, and their acetylderivatives). The conjunction of all this changes greatly diminishes the antimitotic and antiproliferative activities, but the maintenance of the keto bridge produces a potent analogue with the unusual 2,3,4-trimethoxyphenyl moiety. (C) 2009 Elsevier Masson SAS. All rights reserved.

引用

页码：588 / 597

页数：10

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