Determination of anticancer and antibacterial activities of disubstituted tacrine derivatives

The present study describes the biological features of disubstituted tacrine derivatives using cell proliferation and cell cytotoxicity assays. The abilities of tacrine derivatives to inhibit microbial growth and to interact with DNA were also investigated. Here, the tested compounds (1-4) exhibited selective antiproliferative activity against the cancer cell lines (IC50 values 1.1 – 38.9 μg/mL) and showed a similar non-toxic property to cells such as positive control (percent cytotoxicity 7% - 27%). Studies on human pathogenic bacteria showed that the novel tacrine analogues exhibited significant antimicrobial activities between concentrations of 31.25 μg/mL and 250 μg/mL. The data show that they can bind to DNA with the groove binding mode with Kb range of 7.4 × 10⁴ - 2.9 × 10⁴ Mˉ¹. As a result, the preliminary data showed that disubstituted tacrine derivatives exhibited effective pharmacological properties.

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