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Across the world, different diseases have been§treated with herbal extracts, based on common and§empiric knowledge. The process of identification of§the active compounds and their synthesis,§optimisation and development for new drug candidates§appropriate for clinical use is described as§Medicinal Chemistry; a discipline merging chemistry§and pharmacology. §This monograph describes a group of active§ingredients from herbal medicines, as a foundation§for the development of new anticancer drugs.§Interactions between with genomic DNA, synthetic§polynucleotides and higher order DNA isoforms (triple§and quadruple helical forms) have been studied.§Rational drug design has been also employed during§this project to elucidate the mode of binding and§novel compounds have been synthesized to provide§precise structure-activity related studies resulting§in a second generation of chemotherapeutic anticancer§agents with improved properties. §This book provides information and protocols for§studying drug-DNA interactions using spectroscopical§and biological techniques; synthesis of flavonoids§and the principles to explore the use of Quantitative§Structure Activity Relationship Studies.