Background: Dibenzofuran ring is a typical heterocyle which is found in many natural sources and its derivatives
exhibit a wide scale of biological applications similar to its analog ring systems; furan and benzofuran.
Methods: Novel N-(2-methoxydibenzofuran-3-yl)-2-aryloxyacetamide derivatives (2a-l) were synthesized and evaluated for
their cytotoxic activity against A549 lung cancer and NIH/3T3 mouse embryofibroblast cell lines. The inhibition percentages of cathepsin D, L, acetylcholinesterase (AChE) and butrylcholinesterase (BuChE) enzymes provoked by the compounds were also determined.
Results and Discussion: Most of the compounds exhibited significant cytotoxicity whose IC50 values were identified lower
than the tested lowest concentration (<3.90 µg/mL). Compounds 2i against cathepsin D and compound 2k against cathepsin
L displayed the highest inhibitory activity. Regrettably, the compounds demonstrated very weak AChE and BuChE inhibition.
Conclusion: Compounds 2b, 2c, 2e, 2i and 2k exhibited the highest antiproliferative activity against A549 cell lines with
selective profile. However, they did not display satisfying results on tested enzymes.