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Synthesis of Some Substituted 6-Phenyl Purine Analogues and Their Biological Evaluation as Cytotoxic Agents

Asligul Kucukdumlu, Meral Tuncbilek, Ebru Bilget Guven, Rengul Cetin Atalay


A series of 6-(4-substituted phenyl)-9-(tetrahydropyran-2-yl)purines 39, 6-(4-substituted phenyl)purines 1016, 9-((4-substituted phenyl)sulfonyl)-6-(4-substituted phenyl)purines 1732 were prepared and screened initially for their in vitro anticancer activity against selected human cancer cells (liver Huh7, colon HCT116, breast MCF7). 6-(4-Phenoxyphenyl)purine analogues 9, 16, 3032, had potent cytotoxic activities. The most active purine derivatives 5–9, 14, 16, 18, 2832 were further screened for their cytotoxic activity in hepatocellular cancer cells. 6-(4-Phenoxyphenyl)-9-(tetrahydropyran-2-yl)-9H-purine (9) had better cytotoxic activity (IC50 5.4 μM) than the well-known nucleobase analogue 5-FU and known nucleoside drug fludarabine on Huh7 cells. The structure–activity relationship studies reported that the substitution at C-6 positions in purine nucleus with the 4-phenoxyphenyl group is responsible for the anti-cancer activity.


Antitumor agents; hepatocellular carcinoma; Heterocycles; Purine derivatives; Structure-activity relationships

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