The effects of some imidazopyrazine derivatives on telomerase inhibition, mtDNA damage and mtDNA copy number

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Küçük Resim

Tarih

2017

Dergi Başlığı

Dergi ISSN

Cilt Başlığı

Yayıncı

University of Istanbul

Erişim Hakkı

info:eu-repo/semantics/openAccess

Özet

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.

Açıklama

Anahtar Kelimeler

Anticancer Drugs, Imidazopyrazine Derivatives, mtDNA Copy Number, mtDNA Damage, Telomerase Inhibition

Kaynak

Acta Pharmaceutica Sciencia

WoS Q Değeri

Scopus Q Değeri

Q4

Cilt

55

Sayı

3

Künye

Mutlu, 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