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

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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, 1H NMR, 13C 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. |

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