Two new sesquiterpenes (1–2) and one new lupane triterpene (3) have been isolated from the roots of Maytenus apurimacensis. The novel β-dihydroagarofurans are the first sesquiterpenes with a basic polyhydroxy skeleton of 15-deoxyalatol and 4,15-dideoxyalatol that show high MDR reversing activity in the protozoan parasite Leishmania tropica.