Background: Although anticancer chemotherapeutics are available in markets, side effects related to
the drugs in clinical use lead to researchers to investigate new drug candidates which are more safe, potent and
selective than others. Chalcones are popular with their anticancer activities with the several reported mechanisms
including inhibition of angiogenesis, inhibition of tubulin polymerization, and induction of apoptosis etc.
Objective: This study was focused on to synthesize of 1-(2,4/2,6-difluorophenyl)-3-(2,3/2,4/2,5/3,4-
dimethoxyphenyl)-2-propen-1-ones (1-8) and investigate their cytotoxic properties with possible mechanism of
Method: The compounds were synthesized by Claisen-Schmidt condensation. The chemical structures were
confirmed by 1H NMR, 13C NMR, DEPT, COSY, HMQC, HMBC, 19F NMR and HRMS. In vitro cytotoxic
effects of the compounds against human tumour cell lines [gingival carcinoma (Ca9-22), oral squamous cell
carcinoma (HSC-2)] and human normal oral cells [gingival fibroblasts (HGF), periodontal ligament fibroblasts
(HPLF)] were evaluated via MTT test.
Results: All compounds had higher cytotoxicity than reference compound 5-Fluorouracil (5-FU). The compounds
3-7 had higher potency selectivity expression values (PSE) than 5-FU and PSE values of the compounds
were over 100. All chalcone derivatives seem good candidates for further studies according to very remarkable
and high PSE values.
Conclusion: It was clearly demonstrated that compound 7 can induce early apoptosis at a concentration of 10
µM and dose-dependent late apoptosis starting at 10 µM. Compound 7 induced cleavage of the apoptosis marker
PARP. The results indicate that new chalcones reported here can promote apoptosis in human tumour cell lines.