Two new bioactive monotetrahydrofuran acetogenins, calamistrins A (1) and B (2), and two known compounds, uvarigrin (3) and uvarigranin (4), have been isolated from the roots of Uvaria calamistrata. The structures of the new compounds were elucidated by spectroscopic and chemical methods. The absolute stereochemistry of the stereogenic centers was established by Mosher ester methodology.