Determination of anticancer and antibacterial activities of disubstituted tacrine derivatives

Yıl 2019, Cilt: 23 Sayı: 5, 824 - 830, 01.10.2019

Salih Ökten , Ali Aydın , Ahmet Tutar

https://doi.org/10.16984/saufenbilder.469273

Cited By: 8

Öz

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.

Anahtar Kelimeler

tacrine, anticancer, cytotoxcity, antibacterial

Kaynakça

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