idarubicin

Idarubicin, a potent anthracycline antileukemic agent, is orally active in its application. It functions by inhibiting topoisomerase II, thus interfering with DNA replication and RNA transcription. Furthermore, Idarubicin induces DNA damage, inhibits DNA synthesis, and suppresses c-myc expression. It also demonstrates inhibitory effects on the growth of bacteria and yeasts [1] [2] [3] [4] [5].

Idarubicin hydrochloride (Zavedos), a hydrochloride salt form of Idarubicin, is a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells ( IC50: 3.3 ng mL).

N,N-Dimethyl-idarubicin is a derivative of Idarubicin and an effective histone eviction agent that does not induce DNA double-strand breaks. This anthracycline molecule also serves as a potent cytotoxic agent suitable for use in cells overexpressing ABCB1 and resistant to doxorubicin.

N,N-Dimethyl-idarubicin-trisaccharide (compound 26) serves as an effective embedding agent. It exhibits notable cytotoxicity toward cells overexpressing ABCG2 and ABCB1, with IC50 values of 19 nM and 32 nM, respectively.