Synthesis of novel 3, 5, 6-trisubstituted triazine derivatives and their biological activity evaluation as potential antitumor and anti-inflammatory agents

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Küçük Resim

Tarih

2016

Dergi Başlığı

Dergi ISSN

Cilt Başlığı

Yayıncı

University of Istanbul

Erişim Hakkı

info:eu-repo/semantics/openAccess

Özet

In this study, new 3, 5, 6-trisubstituted 1, 2, 4-triazine derivatives (1-9) were synthesized and their structures were determined by using NMR, IR and Mass spectroscopic methods. In vitro antitumor activities against MCF-7 breast adenocarcinoma and C6 rat glioma cell lines were evaluated via MTT colorimetric assay. Among the compounds, compound 4 (IC50=21.0 µg/mL) was found as the most active one against C6 cell line, whereas compound 5 (IC50=9.5 µg/mL) was found the most potent compound against MCF-7 cell line and both of compounds had higher activity than cisplatin in their line. Furthermore, IC50 value of compound 6 was found as 26.0 µg/mL against C6 which was very close to cisplatin potency (IC50=23.5 µg/mL). Besides, all compounds were tested to determine their lipoxygenase (LOX) inhibitory activity. Compounds 1 and 6 showed LOX inhibition with percentages of 43.35% and 38.79% at 100 µg/mL concentration, respectively. The obtained results on cell lines inspire to synthesise new and more potent molecules compounds as anticancer agents.

Açıklama

Anahtar Kelimeler

Antitumor, Cytotoxicity, Lipooxygenase (LOX) Inhibition, Triazine

Kaynak

Acta Pharmaceutica Sciencia

WoS Q Değeri

Scopus Q Değeri

N/A

Cilt

54

Sayı

1

Künye

Yurttaş, L., Şahin, Z., Çiftçi Akalın, G., Temel Edip, H. ve Demirayak, Ş. (2016). Synthesis of novel 3, 5, 6-trisubstituted triazine derivatives and their biological activity evaluation as potential antitumor and anti-inflammatory agents. Acta Pharmaceutica Sciencia, 54(1), 83-92. https://dx.doi.org/10.23893/1307-2080.APS.0547