Investigating the anti-proliferative activity of styrylazanaphthalenes and azanaphthalenediones

被引：43

作者：

Mrozek-Wilczkiewicz, Anna ^{[2
,4
]}

Kalinowski, Danuta S. ^{[1
,3
]}

Musiol, Robert ^{[2
]}

Finster, Jacek ^{[2
]}

Szurko, Agnieszka ^{[4
,5
]}

Serafin, Katarzyna ^{[2
]}

Knas, Magdalena ^{[2
]}

Kamalapuram, Sishir K. ^{[1
,3
]}

Kovacevic, Zaklina ^{[1
,3
]}

Jampilek, Josef ^{[6
,7
]}

Ratuszna, Alicja ^{[4
]}

Rzeszowska-Wolny, Joanna ^{[5
]}

Richardson, Des R. ^{[1
,3
]}

Polanski, Jaroslaw ^{[2
]}

机构：

[1] Univ Sydney, Dept Pathol, Sydney, NSW 2006, Australia

[2] Univ Silesia, Inst Chem, Dept Organ Chem, PL-40006 Katowice, Poland

[3] Univ Sydney, Bosch Inst, Sydney, NSW 2006, Australia

[4] Univ Silesia, Inst Phys, Dept Solid State Phys, PL-40007 Katowice, Poland

[5] M Sklodowska Curie Mem Inst, Ctr Oncol, Dept Expt & Clin Radiobiol, PL-44101 Gliwice, Poland

[6] Zentiva AS, CZ-10237 Prague 10, Czech Republic

[7] Univ Vet & Pharmaceut Sci, Fac Pharm, Dept Chem Drugs, CZ-61242 Brno, Czech Republic

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 07期

基金：

英国医学研究理事会; 澳大利亚研究理事会;

关键词：

Anti-proliferative activity; Quinazolinone; Styrylquinazoline; BIOLOGICAL-ACTIVITY SPECTRUM; INTEGRASE INHIBITORS; ANTITUMOR-ACTIVITY; HIV-1; REPLICATION; ANALOGS; LAVENDAMYCIN; DERIVATIVES; EFFICIENT; AGENTS; ESTER;

D O I：

10.1016/j.bmc.2010.02.025

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A group of styrylazanaphthalenes and azanaphthalenediones were synthesized and tested for their anti-proliferative activity. Most of the compounds were obtained with the use of microwave-assisted synthesis. The lipophilicity of the compounds was measured by RP-HPLC and their anti-proliferative activity was assayed against the human SK-N-MC neuroepithelioma and HCT116 human colon carcinoma cell lines. Active compounds were also tested in clonogenity and comet assays. Several quinazolinone and styrylquinazoline analogues were found to have markedly greater anti-proliferative activity than desferoxamine and cis-platin. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：2664 / 2671

页数：8

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