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In the search of cytotoxic dihydrochalcones, this investigation led to the isolation of seven compounds ( 1 - 7 ) from Eriosema glomeratum and the preparation of eight derivatives ( 8 - 15 ). The cytotoxicity of samples was evaluated against lung (A549), breast (MCF-7), and cervical (HeLa) human cancer cells. The CH 2 Cl 2 /MeOH extract of the aerial part had strong cytotoxicity against all cells [IC 50 11.2 (MCF-7), 8.4 (HeLa) and 13.1 (A549) μg/mL]. A strong activity was also displayed by the n -hexane fraction on MCF-7 (IC 50 11.2 μg/mL). The precursor 3 and the derivative 8 were specifically found as strong cytotoxic agents toward MCF-7 (7.6 μM) and HeLa (3.1 μM), respectively and were more effective than the positive control. Derivatives 8 (3.1 μM) and 9 (21.3 μM) against HeLa were most potent than their precursor 3 (23.7 μM). This is the first preparation of 8 - 14 as well as the cytotoxicity of 3 , 4 , 8 - 15 , fractions, and extract.