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BMH-21 is a planar heterocyclic small molecule DNA intercalator with inhibition of Pol I activity at IC50 = 0.06 μM. [1]

DNA interaction is a well-recognized property for several classes of cancer drugs, which interact with the duplex DNA with three typical binding modalities, namely DNA intercalation, groove binding and covalent interactions. [1]

BMH-21 intercalated into dsDNA and had binding preference towards GC-rich DNA sequences. BMH-21 had wide cytotoxic activities against human cancer cell lines, and acted in p53-independent manner, widely considered as a mediator of many cytotoxic agents. BMH-21 played as a novel agent that inhibited transcription of RNA polymerase I (Pol I) by binding to ribosomal (r) DNA that caused Pol I blockade and degradation of the large catalytic subunit of Pol I, RPA194. BMH-21 led to the dissolution of the nucleolar structure. [1] BMH-21 clearly induced p53 expression in the epithelial compartment of human prostate tissues indicating tissue permeability. [2]

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