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
收藏
页码：2664 / 2671
页数：8
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