Design, synthesis and antiproliferative activity of novel aminosubstituted benzothiopyranoisoindoles

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 mu M range indicating an interesting structure-activity relationship. (C) 2011 Elsevier Ltd. All rights reserved.