title: Design, synthesis and antiproliferative activity of novel aminosubstituted benzothiopyranoisoindoles.
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.
authors: Division of Pharmaceutical Chemistry, Department of Pharmacy, University of Athens, Panepistimiopolis-Zografou, Athens 15771, Greece.
authors: Antonios
authors: A
authors: Christodoulou
authors: Ioannis K
authors: IK
authors: Kostakis
authors: Vassilios
authors: V
authors: Kourafalos
authors: Nicole
authors: N
authors: Pouli
authors: Panagiotis
authors: P
authors: Marakos
authors: Ioannis P
authors: IP
authors: Trougakos
authors: Ourania E
authors: OE
authors: Tsitsilonis
mesh_terms: D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D015195:Drug Design; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D009564:Nitracrine / Q000737:chemistry; D011714:Pyrans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000588:Amines; D000970:Antineoplastic Agents; D007211:Indoles; D011714:Pyrans; D013438:Sulfhydryl Compounds; D009564:Nitracrine