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Description

A potent, 2H-chromen-2-one small molecule inhibitor that is selective for TOP2 (IC50 = 2.8 µ,M and 0.42 µ,M for TOP2alpha and TOP2beta, respectively). Unlike TOP2 poisons such as etoposide, it does not lead to DNA damage associated with DNA Double-Strand Breaks, as evidenced by the lack of gamma-H2AX accumulation but instead inhibits kinetoplast DNA decatenation in vitro. This compound affects cell cycle at the M phase and disturbs mitotic spindle formation in HeLa cells at 3-10 µ,M. It also exhibits significant anti-proliferative activities against several human cancer cell lines.