Synthesis, DNA-damaging and cytotoxic properties of novel topoisomerase II-directed bisantrene analogues

  • Bioorg Med Chem Lett. 1998 Jan 20;8(2):121-6. doi: 10.1016/s0960-894x(97)10207-4.
G Zagotto  1 ,  A Oliva ,  F Guano ,  E Menta ,  G Capranico ,  M Palumbo
Affiliations
  • 1. Department of Pharmaceutical Sciences, University of Padova, Italy.
PMID: 9871638 DOI: 10.1016/s0960-894x(97)10207-4
Abstract

New bisantrene analogues were synthesized, bearing one or two 4,5-dihydro-1H-imidazol-2-yl hydrazone side chains at positions 1,4 or 9 of the anthracene ring system. A 10-azabioisostere was also prepared. The position of substituents in structurally isomeric drugs modulates Topoisomerase II poisoning and specificity, along with cytotoxicity.