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

Bioorganic & Medicinal Chemistry Letters
Isamu ShiinaYoshimune Hasome

Abstract

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.

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Citations

Dec 11, 2013·European Journal of Medicinal Chemistry·Makoto HasegawaTamio Mizukami
Oct 15, 2013·Chemical Biology & Drug Design·Vivian I BonanoSilvia R B Uliana
Apr 12, 2013·Biological & Pharmaceutical Bulletin·Wen-zhi GuoTakao Yamori
Jul 18, 2018·Biomedical Reports·Go HasegawaMotoyuki Shimonaka

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Apoptosis

Apoptosis is a specific process that leads to programmed cell death through the activation of an evolutionary conserved intracellular pathway leading to pathognomic cellular changes distinct from cellular necrosis