Design, synthesis and antiproliferative activity of novel aminosubstituted benzothiopyranoisoindoles

  • Bioorg Med Chem Lett. 2011 May 15;21(10):3110-2. doi: 10.1016/j.bmcl.2011.03.021.
Antonios Christodoulou  1 ,  Ioannis K Kostakis ,  Vassilios Kourafalos ,  Nicole Pouli ,  Panagiotis Marakos ,  Ioannis P Trougakos ,  Ourania E Tsitsilonis
Affiliations
  • 1. Division of Pharmaceutical Chemistry, Department of Pharmacy, University of Athens, Panepistimiopolis-Zografou, Athens 15771, Greece.
PMID: 21444205 DOI: 10.1016/j.bmcl.2011.03.021
Abstract

The synthesis of a number of new benzothiopyrano[4,3,2-cd]isoindole aminoderivatives designed as structural analogues of the key metabolite of the Anticancer agent Ledacrine (nitracrine) and their in vitro cytotoxic activity evaluation against HCT-116, MES-SA, and MES-SA/Dx Cancer cell lines is reported. The majority of the derivatives possessed noticeable cytotoxicity in a low μM range indicating an interesting structure-activity relationship.