Abstract:

The development of new bioactive compounds is necessary to address diseases that have few or no treatments. Diversity-oriented synthesis (DOS) helps in identifying hits and lead compounds, based on the prototypes with known biological activity. Natural products are good sources of bioactive compounds that can be used to design new drugs. The recently described carbazole alkaloid Clauraila A (Fig. 1), isolated from Clausena harmandiana, is a typical example of the prototype compound that allows researchers to study structure-activity relationships for exploring the well-established cytotoxicity against human cell lung cancer. The DOS strategy can be used to develop a carbazole library of Clauralia A analogs and thus diversify the building blocks for synthesizing heterocyclic derivatives. Herein, we have optimized the synthesis of Clauraila A and analogs, with the aim of creating a carbazole library.