Study of dna binding and cytotoxic activity of a benzochromene derivative

Mina Hanifeh ahag,1 Gholamreza dehghan,2,* Majid mahdavi,3



Dna is currently a target for some of the drugs used in cancer therapy. among the various treatment strategies for removing the cancer cells through dna damage, the view of using small agents, capable of binding to dna and oxidative or hydrolytic dna cleavage as anticancer drugs, is an effective method in chemotherapy. the small molecules are capable of binding to dna in non-covalent interaction such as electrostatic binding, groove binding and intercalative binding.


The k562 cell line was obtained from pastor institute of iran (tehran, iran), calf thymus dna (ctdna) was purchased from sigma-aldrich chemical co. the binding mechanism of a benzochromene derivative with calf thymus dna (ctdna) was investigated using uv-vis absorption spectroscopy. cell viability was determined using mtt assay in k562 cells, at different time intervals with and without treatment of the compound.


The result indicate that this compound can interact with dna through non-intercalative mode and the intrinsic binding constant (kb) was estimated to be 2.5 × 103 m-1. furthermore, anti-proliferative and apoptotic effects of the compound was investigated in the human chronic myeloid leukemia k562 cells. this compound affected viability of the treated cells in a time-dependent manner, with ic50 value of 30 µm.


These data indicate that benzochromene derivative is a potent chemotherapeutic agent for chronic myeloid leukemia, and effectively bind to double helix dna through non-intercalative mode. further studies are required to determine whether this compound induses apoptosis or necrosis in k562 cell line.