ACTA Pharmaceutica Sciencia 2016 , Vol 54 , Num 1
Synthesis of novel 3, 5, 6-trisubstituted triazine derivatives and their biological activity evaluation as potential antitumor and anti-inflammatory agents
Leyla Yurttaş 1 Zafer Şahin 2 Gülşen Akalın Çiftçi 3 Halide Edip Temel 3 Şeref Demirayak 2
1 1Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Eskişehir, Turkey
2 2Medipol University, School of Pharmacy, Department of Pharmaceutical Chemistry, İstanbul, Turkey
3 3Anadolu University, Faculty of Pharmacy, Department of Biochemistry, Eskişehir, Turkey
DOI : 10.23893/1307-2080.APS.0547 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 ?g/mL) was found as the most active one against C6 cell line, whereas compound 5 (IC50=9.5 ?g/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 ?g/mL against C6 which was very close to cisplatin potency (IC50=23.5 ?g/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 ?g/mL concentration, respectively. The obtained results on cell lines inspire to synthesise new and more potent molecules compounds as anticancer agents. Keywords : Triazine, cytotoxicity, antitumor, lipooxygenase (LOX) inhibition

Istanbul Medipol University