Ethyl acetate soluble fraction of methanolic extract of Launaea nudicaulis was subjected to chromatographic purification to get four new compounds including a quinic acid derivative (1), a pentahydroxy acetylene analog: trideca-12-ene-4,6-diyne-2,8,9,10,11-pentaol (2), a flavone glycoside (3) and a sesquiterpene lactone (4) together with 10 known compounds. The structures of the new isolates were established by using 1D, 2D NMR techniques and high-resolution mass spectrometry, whereas, the known isolates were identified based on 1D NMR and mass spectrometric information and in comparison with the reported data in the literature. The structure of 4 was also confirmed through single X-ray crystallographic analysis. Cholistaquinate (1) exhibited significant activity in DPPH free radical scavenging assay with an IC50 value of 60.7μM, whereas, nudicholoid (4) exhibited a moderate inhibitory activity against the enzyme butyrylcholinesterase with an IC50 value of 88.3μM.