Synthetic Approaches and Challenges to Transcription Factor Inhibitors

This chapter covers the synthesis and the synthetic challenges associated with representative examples of each of the following classes of transcription factor inhibitors: cyclin dependent kinase (synthesis of flavopiridol), STAT3 (phosphonodifluoromethyl isosteric analogue of a peptidomimetic including its pivaloyloxymethyl pro-drug), STAT5b (Stafib-1), c-Myc–Max (substituted benzanilide) and HIF-1 (Manassantin A). Synthetic approaches to pyrrolobenzodiazepines and diversity-orientated synthesis of transcription factor inhibitors are also discussed.