Synthesis and antitumor activities of piperazine- and cyclen-conjugated dehydroabietylamine derivatives

Abstract

Abstract A series of piperazine- and cyclen-conjugated dehydroabietylamine derivatives were synthesized and characterized by 1H NMR, 13C NMR, and HRMS. The in vitro antitumor activities of conjugates 10–13 against MCF-7 and HepG-2 tumor cell lines were evaluated using CCK-8 assay. The results show that the synthesized compounds cause a dose-dependent inhibition of cell proliferation and display different antitumor activities with the IC50 values ranging from 23.56 to 78.92 μm. Moreover, the antitumor activity of conjugate 10 against the MCF-7 cell line is superior to that of the positive control 5-fluorouracil. In addition, flow cytometric assay revealed that the representative conjugate 10 could induce apoptosis in MCF-7 tumor cells in a dose-dependent manner.