الفهرس 
Synthesis of certain benzimidazole and benzothiazole derivatives expected to have antitumor activity
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Abstract
This thesis comprises five chapters. The first chapter is the introduction, which consists of a brief survey on the pharmacology and chemistry of both benzimidazole and benzothiazole derivatives. The second chapter deals with the aim of the work to achieve synthesis of new anticancer agents. Moreover, it includes schemes that have been carried out to obtain the new required derivatives. The third chapter comprises the discussion part, which reveals theoretical discussion of the experimental work for the synthesis of I and II. Compound II was further reacted to yield diazo coupling derivatives III and IVa-d. Dimer of benzimidazoles Va-c were obtained by one pot reaction of 2- aminobenzimidazole with different acid chlorides. Furthermore, reaction of 2-aminobenzmidazole with oxalyl dichloride and chloroacetyl chloride gave two intermediates VI, VIII which reacted with the appropriate aromatic amine to afford the corresponding derivatives VIIa,b and IX. 2-([1,3]benzothiazol-2-yl)acetonitrile (X) was synthesized by reaction of 2-aminothiophenol and malononitrile and used for the synthesis of X1a-d. Compound X1b was further reacted with o-phenylenediamine and o-aminothiophenol to produce XII, XIII. Finally, X1c reacted with different aldehydes and aromatic amines and yielded XIVa-e and XVa-g respectively. The fourth chapter consists of the experimental part of this work which contains the detailed procedures used for the synthesis of substituted benzimidazoles I, III, IVa-d, Va-c, VIIa,b, IX and benzothiazoles XIa-b, XII, XIII, XIVa-e, XVa-g. The structure of the ii new compounds was confirmed by elemental analyses, IR, 1H NMR, 13C NMR, and mass spectral data. The fifth part includes the evaluation of the cytotoxic activity for all the newly synthesized compounds against human MCF-7 cancer cell line with IC value determination. In addition, it contains Antioxidant 50 Enzyme Assays, Oxidative Stress Assays and Estimation of Nucleic Acids and Protein for the five most active compounds. Compounds Va, VIIb, XIa-d, XII, XIII, XIVa, XIVc, XIVd, XIVe, XVb, XVd, XVe and XVg were found to have potent cytotoxic activity. In addition, the thesis contains a list of one hundred and eighty four references.