Antiproliferative potency of novel benzofuran-2-carboxamides on tumour cell lines: Cell death mechanisms and determination of crystal structure

被引：53

作者：

Hranjec, Marijana ^{[1
]}

Sovic, Irena ^{[1
]}

Ratkaj, Ivana ^{[2
]}

Pavlovic, Gordana ^{[3
]}

Ilic, Natasa ^{[2
]}

Valjalo, Linda ^{[1
]}

Pavelic, Kresimir ^{[2
]}

Pavelic, Sandra Kraljevic ^{[2
]}

Karminski-Zamola, Grace ^{[1
]}

机构：

[1] Univ Zagreb, Dept Organ Chem, Fac Chem Engn & Technol, HR-10000 Zagreb, Croatia

[2] Univ Rijeka, Dept Biotechnol, HR-51000 Rijeka, Croatia

[3] Univ Zagreb, Dept Appl Chem, Fac Text Technol, HR-10000 Zagreb, Croatia

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 59卷

关键词：

Benzofuranes; Carboxamides; Antiproliferative activity; Apoptosis; Crystal structure determination; DERIVATIVES; ANALOGS;

D O I：

10.1016/j.ejmech.2012.11.009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this manuscript the synthesis and biological activity of novel heterocyclic derivatives of benzofuran-2-carboxamides 3a-j and 6a-f is presented. Biological evaluation in vitro revealed that only few compounds exerted concentration-depended antiproliferative effects on tumour cell lines at micromolar concentrations. In particular, 2-imidazolynyl substituted compound 6f showed selectivity on SK-BR-3 cell line while 2-N-acetamidopyridyl substituted 3h and 2-imidazolynyl substituted amide 3i showed selective concentration-dependent antiproliferative effects on SW620 cell line. Compounds 3h and 61 induced apoptosis while compound 3i acted through a cell death mechanism other than apoptosis. (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：111 / 119

页数：9

共 23 条

[1] Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles [J].