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
Affiliations
  • 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.