The effects of some imidazopyrazine derivatives on telomerase inhibition, mtDNA damage and mtDNA copy number
YazarMutlu, Ayşe Gül
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KünyeMutlu, A. G., Bilginer, A., Kayağil, İ., Yıldız, H., Bayhan, Ü., Yılmaz, İ. ... Demirayak, Ş. (2017). The effects of some imidazopyrazine derivatives on telomerase inhibition, mtDNA damage and mtDNA copy number. Acta Pharmaceutica Sciencia, 55(3), 31-41. https://dx.doi.org/10.23893/1307-2080.APS.05517
Imidazopyrazine derivatives have been studied for their curative effects on some diseases like cancer and neurological problems; also, some of these molecules have been patented. Primary human cells exhibit limited replicative potential but the cancer cells divided unlimitedly with passage in culture. This immortality is mainly a result of telomerase activity. We investigated the possible telomerase inhibitor effect and possible mtDNA damage action of five imidazopyrazine derivatives. Telomerase activities were measured by the PCR-ELISA based TRAP method and mtDNA damage assays were achieved by quantitative PCR. We used zebrafish as a model organism for our research. In the application of 6-(4-Metylphenyl-8-(4-chlorophenyl)imidazo[1,2-a]pyrazine (C19H14N3Cl), it was determined that this compound inhibit telomerase activities to a statistically significant degree. The obtained results from molecular docking studies also supported the experimental results. Accordingly, this compound has the probability to be used as an anti-cancer agent after detailed studies.