Conformationally restricted macrocyclic analogues of combretastatins

被引：12

作者：

Mateo, Carmen ^{[1
]}

Alvarez, Raquel ^{[1
]}

Perez-Melero, Concepcion ^{[1
]}

Pelaez, Rafael ^{[1
]}

Medarde, Manuel ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 22期

关键词：

combretastatins; conformational restriction; macrocycles; tubulin polymerization inhibition;

D O I：

10.1016/j.bmcl.2007.08.075

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New analogues of combretastatins have been evaluated as inhibitors of tubulin polymerization. These compounds present a macrocyclic structure, in which the para positions of the aromatic moieties have been linked by a 5- or 6-atoms chain, in order to produce a conformational restriction. This could contribute to determine the active conformation for these ligands. Such a conformational restriction and/or the steric hindrance makes them less potent inhibitors than the model compound CA-4. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：6316 / 6320

页数：5

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