Many cancer cells over-express receptors for certain vitamins such as folic acid and biotin, therefore attaching one of these vitamins to a cytotoxic compound (e.g. cisplatin) is a potential method for designing useful chemotherapeutic agents with increased selectivity and cellular uptake. The research presented herein will detail our work towards the synthesis of biotinylated imidazophenanthroline and dipyridophenazine-based platinum complexes. Synthetic strategies for the coupling of 1,10-phenanthroline-5,6-dione to 4-acetylaminobenzaldehyde and 1,2,4-triaminobenzene compounds will be discussed along with an EDC-mediated biotin coupling scheme. The bioactivities of the compounds against HCT-15 cancer cells will be explored and the results presented and discussed.

Synthesis and biological testing of biotinylated dione-coupled platinum complexes

245th National Meeting (2013)

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