2. Academic Validation
  3. Pyrroloquinolinone-based dual topoisomerase I/II inhibitor

Pyrroloquinolinone-based dual topoisomerase I/II inhibitor

  • Eur J Med Chem. 2014 Apr 22:77:103-9. doi: 10.1016/j.ejmech.2014.02.064.
Lisa Dalla Via 1,  Giovanni Marzaro 1,  Alessandro Ferrarese 1,  Ornella Gia 1,  Adriana Chilin 2
Affiliations

Affiliations

  • 1 Dipartimento di Scienze del Farmaco, Università degli Studi di Padova, Via Marzolo 5, 35131 Padova, Italy.
  • 2 Dipartimento di Scienze del Farmaco, Università degli Studi di Padova, Via Marzolo 5, 35131 Padova, Italy. Electronic address: adriana.chilin@unipd.it.
PMID: 24631729 DOI: 10.1016/j.ejmech.2014.02.064
Abstract

A new series of pyrroloquinolinones bearing different alkylamino side chains were synthesized and evaluated as cytotoxic compounds against three different human tumor cell lines (HeLa, HL-60 and A431). Some compounds showed interesting antiproliferative activity, in particular against A431 cells. The compounds were tested for their ability to counteract Topoisomerase II relaxation activity and the most interesting one (3c) was tested also against Topoisomerase I, resulting a dual inhibitor. The molecular interactions between 3c and the intracellular targets were finally investigated through molecular modeling simulations.

Keywords

Dual activity; Molecular docking; Pyrroloquinolinone; Topoisomerase.

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