For the development of new antitumor agents, novel dibenzo-1,7-diaza-14-crown-4 ethers containing γ-piperidone moiety and diazacrown ether fragments were synthesized by a domino condensation of new podands (4a,b), simple ketones and ammonium acetate. Four diazacrown ethers were evaluated in vitro test for cytotoxic activity against 5 human cancer cell lines: Hep-G2, RD, MCF-7, Lu1, HeLa and the Vero cell line. X-Ray structural analysis was performed to determine the structure of the representative compound 6a.