Benzoquinazoline derivatives as new agents affecting DNA processing

  • Bioorg Med Chem. 2011 Feb 1;19(3):1197-204. doi: 10.1016/j.bmc.2010.12.037.
Giovanni Marzaro  1 ,  Lisa Dalla Via ,  Antonio Toninello ,  Adriano Guiotto ,  Adriana Chilin
Affiliations
  • 1. Department of Pharmaceutical Sciences, University of Padova, Via Marzolo 5, 35131 Padova, Italy.
PMID: 21216603 DOI: 10.1016/j.bmc.2010.12.037
Abstract

A new series of benzo[h]quinazoline and benzo[f]quinazoline derivatives was prepared and studied for the biological activity. The compounds carrying a dimethylaminoethyl side chain (6c, 8c and 12) inhibit cell growth. The ability to form a molecular complex with DNA and to interfere with topoII and topoI relaxation activity was evidenced for the most active 6c and 8c, along with the capacity to induce Apoptosis on HeLa cells.