Background: Dibenzofuran ring is a typical heterocyle that 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.
Materials and 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). Compound 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