ISSN : 0970 - 020X, ONLINE ISSN : 2231-5039
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Abstract

Synthesis Novel Fluorinated Cyclic Nanomeric Aza Crown Macrocyclic System Containing 1,2,4-Triazine Moiety and Ru-Complex as CDK2 Inhibitors of Tumor Cells (Protection of DNA Damage)-Part II

Wafa A. Bawazir* and Reda M. Abdel-Rahman

DOI : http://dx.doi.org/10.13005/ojc/360614


Abstract:

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.H2O 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).

Keywords:

CDK2 Inhibitors; Fluorinated Aza-Crown; Nanomeric: Ru-Complex; 1,2,4-Triazine

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