Synthesis of the new pseudo-symmetrical tamoxifen derivatives and their anti-tumor activity

Three new pseudo-symmetrical tamoxifen derivatives, RID-B (15), C (16), and D (17), were synthesized via the novel three-component coupling reaction, and the structure–activity relationships of the pseudo-symmetrical tamoxifen derivatives were examined. It was discovered that 15 strongly inhibits the viability of HL-60 human acute promyelocytic leukemia, whereas 16 possesses medium activity against the cell line and 17 has no effect on the cell viability. The agarose gel electrophoresis for DNA cleavage showed the cell death might be induced by apoptosis.

Graphical abstractThe synthesis of new tamoxifen derivatives is reported. Their effects on growth of HL-60 cells are determined.Figure optionsDownload full-size imageDownload as PowerPoint slide