Design, synthesis, photophysical and biological evaluation of Novel 1,8-naphthalimide derivatives as DNA binders and potential anti-cancer agents

Abstract

This thesis, titled 'Design, Synthesis, Photophysical and Biological Evaluation of Novel 1,8-Naphthalimide Derivatives As DNA Binders and Potential Anti-Cancer Agents' is divided into seven chapters. The first chapter is an introduction to the discovery and the progression of 1,8-naphthalimides as anticancer agents. This research represents an im portant contribution to the design of potent therapeutic agents, some of which have entered clinical trial. For example, Quinamed® developed by GhemGenex Pharmaceutica, has been shown to be active in Gleevec resistant patients with prostate cancer. This Chapter also deals with the utility of DNA cleaving proteins for achieving greater sequence specificity in DNA binding, and on the natural occurrence of thiazole and oxazole containing cytotoxic cyclic peptides. The final section of Chapter 1, reviews the properties and the applications of synthetic Troger's base derivatives, which in the past have been used as receptors, as well as chiral solvating agents. Despite the many highly desirable properties of the Troger's base, there only exist a few reports on its incorporation into known DNA-binding motifs.