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

Abstract

A series of piperazine- and cyclen-conjugated dehydroabietylamine derivatives were synthesized and characterized by 1 H NMR, 13 C 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 IC 50 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.