Concise Synthesis of Benzoindolizidine Derivatives and Bioactivity Evaluation

Due to the profound cytotoxicities and interesting biochemical aspects, phenanthroindolizidine alkaloids have received attention as potential therapeutic leads. To define the features of the molecule that are essential for their excellent bioactivities, we have synthesized two hexahydropyrrolo[1,2-b]isoquinolines and their hydrochloride salts and picrates concisely and evaluated their antiviral and anticancer activities. We found that the replacement of the phenanthrene with a benzene in phenanthroindolizidine alkaloids observably decreased their antiviral and anticancer activities, and thus the phenanthrene in phenanthroindolizidine alkaloids is essential for high antiviral and anticancer activities.