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ACTA Pharmaceutica Sciencia 2017 , Vol 55 , Num 3
The Effects of Some Imidazopyrazine Derivatives on Telomerase Inhibition, mtDNA Damage and mtDNA Copy Number
Ayşe Gül Mutlu 1 Abdulkerim Bilginer 2 Ismail Kayağil 3 Hülya Yıldız 2 Ülkü Bayhan 4 İnanç Yılmaz 4 Şeref Demirayak 5
1 Mehmet Akif Ersoy University, Arts and Sciences Faculty, Department of Molecular Biology and Genetics, Burdur, Turkey
2 Mehmet Akif Ersoy University, Arts and Sciences Faculty, Department of Biology, Burdur, Turkey
3 Mehmet Akif Ersoy University, Arts and Sciences Faculty, Department of Chemistry, Burdur, Turkey
4 Mehmet Akif Ersoy University, Arts and Sciences Faculty, Department of Physics, Burdur, Turkey
5 Medipol University, Faculty of Pharmacy, İstanbul, Turkey
DOI : 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. Keywords : Imidazopyrazine derivatives, Telomerase inhibition, mtDNA damage, mtDNA copy number, anticancer drugs

Istanbul Medipol University