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Abstract N-containing heterocycles are still an important resource for the discovery of new drugs. The acridine ring system occurs in various natural products, especially in alkaloids. The acridine core is often used for the design of many synthetic compounds with diverse pharmacological properties. This thesis deals with the synthesis and biological evaluation of some new acridine derivatives as anticancer agents and includes three chapters. The first chapter is the introduction which comprises an updated literature survey on the chemistry and biological application of acridine and its derivatives. This review included the design and synthetic strategies used to obtain the acridine derivatives, as well as, their reactions and biological applications are reviewed and discussed. The second chapter is devoted to results and discussion which includes the design, and synthetic methodologies of the 9-substituted acridine derivatives. In addition, compounds characterization and plausible mechanism which led to the formation of the key products are discussed. Moreover, in vitro anticancer activity was described. Herein, we report the synthesis and biological evaluation of new acridine derivatives with substitution pattern at 9th position. The route of preparation of N-phenylanthranilic acid, the starting intermediate for the synthesis of 9-chloroacridine, was based on modified Ullmann- Goldberg reaction which involves reaction of o-chlorobenzoic acid dissolved in DMF with aniline in presence of sodium acetate as base and copper as cocatalyst for 6-8 h. 9-chloroacridine, was obtained in good yield through cyclization and dehydroxy chlorination reaction of N-phenylanthranilic acid with freshly distilled phosphorous oxychloride under reflux for 8-12 h as depicted in Scheme 1. |