Saturday, August 4, 2012

Phenanthriplatin, a monofunctional DNA-binding platinum anticancer drug candidate with unusual potency and cellular activity profile

  1. Stephen J. Lippard

A set of monofunctionalized platinum complexes were synthesized with the general formula: cis-[Pt(NH3)2(N-heterocycle)Cl]Cl. In particular, complexation to phenanthridin showed enhanced cytotoxic behaviour compared to other tested N-heterocycles, cisplatin, or oxaliplatin. Cellular uptake was shown to be higher likely as a result of the N-heterocycle. As well, in studies comparing binding of these complexes with 5'-deoxyguanosine monophosphate and N-acetyl methionine, the phenanthridin showed better binding to the nucleotide suggesting it might overcome drug resistance that results from interactions with sulfur based compounds.

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