الفهرس | Only 14 pages are availabe for public view |
Abstract In this investigation, the behavior of chromone derivatives towards some nucleophiles was studied aiming to construct several heterocycles and to evaluate their antitumor activity. The work of this thesis consists of three parts: Part I: This part deals with the behavior of 3-formylchromone derivative 3 towards some carbon and nitrogen nucleophiles e.g., 2,4-dioxothiazolidine, 5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, ethyl cyanoacetate, acetylacetone, 4-aminopyridine, p-aminoacetophenone, methyl-p-aminobenzoate, thiosemicarb-azide and hydrazine hydrate. Evaluation of the anticancer activity of the synthesized compounds against different human cancer cell lines including breast (MCF-7), colon (HCT116), lung (A549), liver (HepG2), prostate (PC3) and human normal melanocyte (HFB4), was investigated.Part II: In this part, the chemoselectivity of the chromonyloxazolone towards some nitrogen nucleophiles has been studied under different reaction conditions in order to construct a variety number of N-heterocycles. The synthesized compounds were screened as anticancer agent against the two cancer cell lines; the breast and the colon, cell lines. Part III: This part presents the heteroannulation reactions of 2-amino-6-chloro-3-formylchromone 40 via microwave assisted reactions of with some carbon nucleophiles involving α-tetralone, 3,5-dimethylbarbituric acid, 2-methyl-2-phenyl-1,3-dioxane-4,6-dione, 2,4-dioxothiazolidine, 5-methyl-2,4-dihydro-3H-pyrazol-3-one, malononitrile, cyanoacetamide, acetylacetone and ethyl cyano-acetate. The former compound was prepared from reaction of 6-chlorochrom-one-3-carboxaldehyde with hydroxylamine hydrochloride in the presence of ammonium hydroxide. Some of the synthesized compounds were screened for their anticancer agent against two cancer cell lines; breast and colon. Keywords: 3-Formylchromone, Benzothiazole, 2,4-Dioxothiazolidine, Oxazol-one, Benzimidazole, Heteroannulated compounds, Antitumor activity. |