Structural Studies of Cytotoxic Marine Alkaloids: Synthesis of Novel Ring-E Analogues of Ascididemin and their in vitro and in vivo Biological Evaluation

The cytotoxic marine alkaloid ascididemin and various pyridine ring-E analogues have been synthesised in an attempt to determine the pharmaceutical utility and structure-activity requirements for the parent alkaloid. All compounds synthesised were evaluated in a wide range of biological screens for selective cytotoxicity, antiviral, antifungal and antimicrobial properties. Many analogues exhibited selective cytotoxicity to human solid tumour cell-lines in vitro, with one also exhibiting moderate antitumour activity in in vivo xenograft assays.