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The development of Py–Im polyamides as potential therapeutic agents is an example of the application of fundamental science at all levels from initial concept, based on purely chemical considerations of DNA–binding, through refinement of the design process to improvements in synthesis, critical analysis of DNA–binding properties, solving problems of cell uptake and distribution, pharmacokinetics and whole–animal studies leading up to clinical trials. This chapter will document the story with particular regard to the development of drugs aimed at treating one of the most prevalent cancers that beset patients today, therapy-resistant prostate cancer.

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