Determination of anticancer and antibacterial activities of disubstituted tacrine derivatives

Abstract

The present study describes the biological features of disubstituted tacrine derivatives by using cell proliferation and cell cytotoxicity assays. The ability of compounds to inhibit microbial growth and to interact with DNA was also investigated. Here, tested compounds exhibit selective antiproliferative activity against the cancer cells (IC₅₀ values 1.1 – 38.9 µg/mL) and show a similar non-toxic property to cells such as positive control (percent cytotoxicity 7% - 27%). Studies on human pathogenic bacteria have shown that the novel compounds exhibit a significant antimicrobial activity between concentrations of 31.25 μg/mL and 250 μg/mL. There is strong data showing that they can bind to DNA with the groove binding mode with a binding constant range of 7.4 x 10⁴ - 2.9 x 10⁴ Mˉ¹. As a result, the preliminary data show that disubstituted tacrine derivatives exhibit effective pharmacological properties.

Keywords

• tacrine,anticancer,cytotoxcity,antibacterial

References

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