Chemical investigation from roots of Enkleia siamensis (Kurz) Nervling resulted in the isolation of 10 compounds. Their structures were established on the basis of 1D and 2D NMR spectroscopic data as linobiflavonoid (1), chamaejasmin (2), 7-O-β-D-glucopyranosylchamaejasmin (3), ormocarpin (4), (-)-wikstromol (5), matairesinol (6), (+)-lariciresinol (7), umbelliferone (8), daphnoretin (9) and carthamidin (10). Compounds 2 and 8 showed cytotoxicity against KB, MCF-7 and NCI-H187 cancer cell lines. Compounds 1, 2 and 5 showed weak minimum inhibitory requirements to acetylcholinesterase with values ranging from 50 to 1000 ng. In addition, compound 2 exhibited antimalarial activity against Plasmodium falciparum with an IC50 value of 2.32 μg/mL.