Synthesis and in vitro anticancer evaluation of 1,4-phenylene-bis-pyrimidine-2-amine derivatives

Authors : Meliha Burcu GÜRDERE, Erdoğan KAMO, Ayşe Şahin YAĞLIOĞLU, Yakup BUDAK, Mustafa CEYLAN

Pages : 263-271

View : 22 | Download : 7

Publication Date : 0000-00-00

Article Type : Research Paper

Abstract :A series of 1,4-phenylene-bis-chalcones 3a-3h were synthesized by the reaction of terephthalaldehyde with substituted arylketones in this study. The novel 1,4-phenylene-bis-pyrimidine-2-amine derivatives 5a-5h were obtained by the addition of guanidine hydrochloride to 1,4-phenylene-bis-chalcone 3a-3h in ethanolic KOH under reflux conditions. The structure of the compounds was explained by means of IR, $^{1}$H NMR, $^{13}$C NMR, and elemental analyses. The anticancer activities of 3a-3h and 5a-5h were investigated against rat brain tumor cells and human uterus carcinoma in vitro$.$ Activity tests were performed as dose-dependent assays at eight concentrations. The positive control was 5-fluorouracil insert ignore into journalissuearticles values(5-FU);. Compounds 3c and 3d were examined and they showed high activities as compared to 5-FU against C6 insert ignore into journalissuearticles values(rat brain tumor); and HeLa insert ignore into journalissuearticles values(human uterus carcinoma); cells. The anticancer activity of 5h was better than that of 5-FU at high concentrations cell-selectively against C6 cells.
Keywords : 1, 4 Phenylene bis chalcone, 1, 4 phenylene bis pyrimidine, HeLa, C6, anticancer activity, 5 fluorouracil