1207435-84-4Relevant academic research and scientific papers
Synthesis, Inhibitory Activity, and in Silico Modeling of Selective COX-1 Inhibitors with a Quinazoline Core
Dvorakova, Marcela,Langhansova, Lenka,Temml, Veronika,Pavicic, Antonio,Vanek, Tomas,Landa, Premysl
supporting information, p. 610 - 616 (2021/04/07)
Selective cyclooxygenase-1 (COX-1) inhibition has got into the spotlight with the discovery of COX-1 upregulation in various cancers and the cardioprotective role of COX-1 in control of thrombocyte aggregation. Yet, COX-1-selective inhibitors are poorly explored. Thus, three series of quinazoline derivatives were prepared and tested for their potential inhibitory activity toward COX-1 and COX-2. Of the prepared compounds, 11 exhibited interesting COX-1 selectivity, with 8 compounds being totally COX-1-selective. The IC50 value of the best quinazoline inhibitor was 64 nM. The structural features ensuring COX-1 selectivity were elucidated using in silico modeling.
Investigating the anti-proliferative activity of styrylazanaphthalenes and azanaphthalenediones
Mrozek-Wilczkiewicz, Anna,Kalinowski, Danuta S.,Musiol, Robert,Finster, Jacek,Szurko, Agnieszka,Serafin, Katarzyna,Knas, Magdalena,Kamalapuram, Sishir K.,Kovacevic, Zaklina,Jampilek, Josef,Ratuszna, Alicja,Rzeszowska-Wolny, Joanna,Richardson, Des R.,Polanski, Jaroslaw
experimental part, p. 2664 - 2671 (2010/06/14)
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.
Investigating biological activity spectrum for novel styrylquinazoline analogues
Jampilek, Josef,Musiol, Robert,Finster, Jacek,Pesko, Matus,Carroll, James,Kralova, Katarina,Vejsova, Marcela,O'Mahony, Jim,Coffey, Aidan,Dohnal, Jiri,Polanski, Jaroslaw
experimental part, p. 4246 - 4265 (2010/03/01)
In this study, series of ring-substituted 2-styrylquinazolin-4(3H)-one and 4-chloro-2-styrylquinazoline derivatives were prepared. The syntheses of the discussed compounds are presented. The compounds were analyzed by RP-HPLC to determine lipophilicity. They were tested for their inhibitory activity on photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the synthesized compounds was also performed against four mycobacterial strains and against eight fungal strains. Several compounds showed biological activity comparable with or higher than that of the standard isoniazid. It was found that the electronic properties of the R substituent, and not the total lipophilicity of the compound, were decisive for the photosynthesis-inhibiting activity of tested compounds.
