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Novel fluorinated 1,5-disubstituted-1,3,5-triazepine-6,7-dione (4) has been obtained from the interaction between 5,6-bis(4-fluorophenyl)-1,2,4-triazine-3-thiol (1) with 2,6-diaminopyridine 2 followed by ring closer reaction with diethyl oxalate. Also, Ru-complex 7 obtained by refluxing of compound 1 with 6-(4-fluorophenyl)-1,2,4-triazine-3,5-diamine (5) to produce compound 6, the later was reacted with RuCl3.xH2O to produce the target 7. Structures of the products deduced from their elemental analysis and spectral measurements. Compounds 3, 4, 6, and 7 were evaluated as CDK2 inhibitors of tumor cells; these compounds exhibited a potential activity against CDK2, where the IC50 values were 4.5, 6.8, 4.0, and 5.0 μM respectively in comparison with Olomoucine standard (IC50=5.0 μM).

oriental journal of chemistry/oriental journal of chemistry

Synthesis Novel Fluorinated Cyclic Nanomeric Aza Crown Macrocyclic System Containing 1,2,4-triazine moiety and Ru-complex as Cyclin-dependent kinase 2 (CDK2) inhibitors of tumor cells (Protection of DNA Damage)-Part II