This chapter will focus on various classes of compounds that possess potent antitumor, antiHIV, and antifungal activity recently discovered in my laboratory. These compounds were obtained by bioactivity-and mechanism of action-directed isolation and characterization

coupled with rational drug design-based modification and analog synthesis. Research highlights include GL331, which is currently in anticancer clinical trials, the antifungal 1,4bis-(2,3-epoxypropylamino)-9,10-anthracenedione, and the anti-HIV coumarin DCK and the triterpene DSB as well as their analogs.