Investigating the anti-proliferative activity of styrylazanaphthalenes and azanaphthalenediones

Bioorg Med Chem. 2010 Apr 1;18(7):2664-71. doi: 10.1016/j.bmc.2010.02.025.

Anna Mrozek-Wilczkiewicz ¹, Danuta S Kalinowski, Robert Musiol, Jacek Finster, Agnieszka Szurko, Katarzyna Serafin, Magdalena Knas, Sishir K Kamalapuram, Zaklina Kovacevic, Josef Jampilek, Alicja Ratuszna, Joanna Rzeszowska-Wolny, Des R Richardson, Jaroslaw Polanski

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1 Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40006 Katowice, Poland.

PMID: 20303768 DOI: 10.1016/j.bmc.2010.02.025

Abstract

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.

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