Approximately half the people treated by chemotherapy for cancer receive a platinum drug.  Only testicular cancer patients can expect a complete cure, a consequence of the remarkable properties of cisplatin, the prototypical member of the class of platinum anticancer drugs.  This presentation will describe our work on a cisplatin derivative, phenthriplatin, in which a chloride ion is replaced by phenanthridine.  The resulting cationic complex forms monofunctional adducts on DNA that block transcription and, in cell-based assays, display a different cancer cell-killing profile from those of the established platinum drugs.  Mechanistic work, including a crystal structure analysis of phenthriplatin-modified DNA in the active site of RNA polymerase II, and the results of animal toxicity and efficacy studies will be presented.  This work was funded by the National Cancer Institute.

Chemical, structural, and biological studies of phenanthriplatin, a monofunctional DNA-damaging agent with anticancer drug potential

243rd National Meeting (2012)

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