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Although often envisaged to be a disease of ancient origin, cancer continues to be a leading cause of death worldwide. Developing anti-cancer therapeutics has long been an active field of research in both academia and industries, providing us with several chemotherapeutic drugs to fight against cancer. However, side effects are inevitable with most of the current anti-cancer therapies and emergence of drug resistance in many cases has also been noted. The need for finding novel anti-cancer targets as well as potent drugs against cancer, therefore, remains still valid. Among potential targets for developing novel anti-cancer drugs, a few oncogenic transcription factors appear to be quite promising. Though traditionally regarded as ‘undruggable’, such a notion has been recently challenged by the growing evidence presenting strategies including small molecules of natural and synthetic origin. This chapter seeks to illustrate molecular targeting of few oncogenic transcription factors using some naturally occurring small molecules.

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