0000000000092748

AUTHOR

A. D’anneo

The synergistic effect exerted by the HDAC inhibitor SAHA and the sesquiterpene lactone parthenolide on triple negative breast canc er cells

Triple-negative breast cancer (TNBC) is a subtype o f breast cancer, insensitive to endocrine therapy. Chemotherapy is the main form of treatment, but is accompanied by a high rate of recidivism. The sesquiterpene lactone Parthenolide (PN) exerts a cy totoxic effect on MDA-MB231 cells, a TNBC cell line (1), but was ineffective at low doses (2-5μM). This repr esents an obstacle for a therapeutic utilization of PN. We supposed, in line with other authors (2), that PN c auses a protective response, which at low doses pre vails on the cytotoxic effect. With the aim of inhibiting this protective effect we have shown that pre-trea tment of MDA-MB231 cells with SAHA (2-5μM), an histone deace tylat…

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Synthesized benzamido derivatives exert antiproliferative effects by DNA damage and ROS generation.

In this study we explored the effect and the biological action of synthesized benzamido derivatives bearing the (1S,2S)-2-phenyl-cyclopropane-1-carboxamido, 1,1'-biphen-2-carboxamido and 1,1'-biphen-4-carboxamido moieties on K562, a human leukemia cell line. Among the synthesized compounds a particular antiproliferative action was observed with the benzamido derivative bearing the 2-1,1'-biphenyl moiety with the substitution at the 5 position of the benzamido moiety with iodine. This compound showed cytotoxic effects in K562 leukemic cells at nanomolar concentrations and was, therefore, chosen as compound to explore its mode of action. Our analyses provided evidence that this benzamido deri…

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