Introduction. The flavonoids represent a large group of polyphenolic compounds containing a benzo-γ-pyrone nucleus in their structure and are broadly found in several plants. These natural products are synthesized via the phenylpropanoid pathway. Several papers described in the literature highlight that secondary metabolites of phenolic nature, including flavonoids, are relationed with a diversity of biological properties. Recent interest in these compounds is based on its potential health benefits derived from the antioxidant activities. Fruits and vegetables presenting flavonoids in their composition have been reported as chemopreventive agents for various cancers.Consumption of onions and/or apples, two main sources of flavanone quercetin, is associated with a reduction in the incidence of prostate, lung, stomach and breast cancer. In addition, moderate wine consumption also allows a lower risk for the development of lung, endometrial, esophagus, stomach and colon cancer. Aim. Due to the antitumor activity described for flavonoids derivatives and considering the importance and necessity of the discovery of new drugs effective for antitumor therapy, this work aims to carry out the preparation of novel compounds derived from 6-hydroxy-flavanone through Williamson synthesis, as well as evaluation of antitumor activity. Methods. 6-hydroxy-flavanone (0.05 g, 0.2 mmol), Potassium carbonate (0.043 g, 0.3 mmol), 3 ml of DMF (Dimethylformamide) or Acetone and a mixture was kept under stirring on an ice bath for 25 minutes. Then functionalized commercial bromide (0.31 mmol). Subsequently the reaction mixture was stirred at room temperature for 4h. Finally, a chromatographic column was performed using a hexane/ether (9:1 or 7:3) as eluent and pure compounds were obtained. Results. Until this moment four 6-hydroxy-flavanone derivatives were prepared in 14-58% yield. All compounds were elucidated by HPLC and 1H NMR spectroscopic analysis. Conclusion. Further reactions in order to prepare novel flavanone derivatives are ongoing as well as antitumor activity evaluation.