Cameroon enjoys a rich biota including a plethora of medicinal plants, which have traditionally been used for hundreds ofyears to treat various ailments, and form the basis of the country’s primary healthcare system. Medicinal plants of thegenera Fagara (F: Rutaceae), and Hannoa and Pierreodendron (F: Simaroubaceae) belong to the Cameroonian flora, andare used by the local people to treat malaria, cancer, rheumatism, bacterial infections, pain, inflammations, typhoid, skininfection and other serious disorders. Previous studies carried out on certain species of these genera afforded variousphytochemicals (quassinoids, furoquinoleine, acridones, cathinone alcaloids, triterpenoids and steroids) and revealedinteresting pharmacological properties (cytotoxicity, antiplasmadial activities). This project proposes to employ acombination of chemical fingerprinting-based dereplication, assay-guided fractionation and reversed-phase preparative highperformance chromatographic methods to identify potential anticancer and antimalarial lead compounds from plants of thegenera mentioned above, selected on the basis of ethnobotanical information as well as literature data. The structures ofthe isolated compounds will be elucidated by spectroscopic means (UV, IR, MS, NMR and X-ray). Structural modification toincrease activity of compounds will be carried out applying modern semisynthetic approaches in order to establish structureactivityrelationships. Total synthesis will also be carried out to increase to quantity of the lead compounds. Suitable in vitrobioassays, relevant to cytotoxicity, antimalarial and toxicity determination will be utilised to aid isolation processes as well asfor the determination of bioactive potencies of the isolated lead compounds. The main objective is to discover and developbioactive natural products and their analogues as clinical trial candidates.