Determination of anticancer and antibacterial activities of disubstituted tacrine derivatives

Abstract

The present study describes the biological features of disubstituted tacrine derivatives using cell proliferation andcell cytotoxicity assays. The abilities of tacrine derivatives to inhibit microbial growth and to interact with DNA werealso investigated. Here, the tested compounds (1-4) exhibited selective antiproliferative activity against the cancercell lines (IC50 values 1.1 – 38.9 ?g/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 analoguesexhibited significant antimicrobial activities between concentrations of 31.25 ?g/mL and 250 ?g/mL. The data showthat they can bind to DNA with the groove binding mode with Kb range of 7.4 10? - 2.9 10? M?¹. As a result, thepreliminary data showed that disubstituted tacrine derivatives exhibited effective pharmacological properties.