الفهرس 
IntroductionOnly 14 pages are availabe for public view
 |  | from | 238 |  |  |
| | | from | 238 | | |
Abstract
The current work is a part of the program that deals with the synthesis of distinctive organic molecules to evaluate their potency as antioxidant, cytotoxic agents, and bleomycin DNA damage. We report in this investigation efficient synthetic routes for the preparation of a series of bicyclic, and binary heterocycles containing pyrmidinione ring systems to assess their biological activity as antioxidant, and anticancer agents.The work in this thesis is divided into two main parts:(1)Synthesis of the Target Heterocyclic Compounds.1.1 Synthesis of Bicyclic 5-6 Heterocycles in which we Synthesis of pyrazolo[3,4-d]pyrimidinones and isoxazolo[5,4-d]pyrimidinones 1.2 Synthesis of Bicyclic 6-6 Heterocycles :- Synthesis of pyrimido[4,5-d]pyrimidinones 1.3 Synthesis of Bicyclic 7-6 Heterocycles :- Synthesis of pyrimido[5,4-f][1,4]oxazepinones, [1,4]oxathiepino[7,6-d]pyrimidinones, and pyrimido[5,4-c]diazepinones. 1.4 Synthesis of Substituted Barbiturates, and Thiobarbiturates 1.5 Binary Heterocycles Based-Pyrimidines :- Synthesis of pyrimidinones and pyrimidinone-based heterocycles(2)Biological Evaluations of the Newly Synthesized Compounds.2.1 Cytotoxicity Activity The cytotoxic effect of the designed compounds has been assessed in vitro at the National Institute of Cancer, Cairo, Egypt on two well-known human cell lines, liver hepatocellular carcinoma (HepG2) and normal lung fibroblast (WI-38). 3-(4,5-Dimethylthiazole-2-yl)-2,5- diphenyl-tetrazolium bromide (MTT) colorimetric assay was applied to investigate the cytotoxic effect of the synthesized compounds. Doxorubicin was used as a chemotherapeutic reference standard for scale comparison. 2.2ABTS Radical Scavenging Assay The antioxidant activity of the investigated pyrimidinones was evaluated by their ability to decolorize the 2,2’-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radical and the corresponding radical-scavenging activity was estimated by the decrease in the absorbance at 734 nm. Ascorbic acid “Vitamin C”, one of the most effective antioxidant agents, was used as a reference standard to compare the results of the tested samples.