Small-molecule Transcription Factor Inhibitors in Oncology
Synthetic Approaches and Challenges to Transcription Factor Inhibitors
Published:05 Sep 2018
Special Collection: 2018 ebook collectionSeries: Drug Discovery
G. Procopiou and P. A. Procopiou, in Small-molecule Transcription Factor Inhibitors in Oncology, ed. K. M. Rahman and D. E. Thurston, The Royal Society of Chemistry, 2018, pp. 1-41.
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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.