1371631-75-2Relevant academic research and scientific papers
Symmetrical Diamidates as a Class of Phosphate Prodrugs to Deliver the 5′-Monophosphate Forms of Anticancer Nucleoside Analogues
Slusarczyk, Magdalena,Ferrari, Valentina,Serpi, Michaela,G?nczy, Blanka,Balzarini, Jan,McGuigan, Christopher
, p. 2305 - 2316 (2018)
The application of phosphorodiamidate technology to pyrimidine and purine nucleosides with anticancer activity to potentially overcome the resistance mechanisms associated with parent nucleosides is reported. Sixteen symmetrical phosphorodiamidates were prepared from the natural amino acids l-alanine and glycine. All the compounds were evaluated for their cytotoxic activity against a wide panel of solid and leukaemic tumour cell lines. In addition, a carboxypeptidase Y assay was performed on a representative phosphorodiamidate in order to reveal the putative bioactivation pathway for the reported phosphorodiamidate-type prodrugs.
PHOSPHORAMIDITE DERIVATIVES OF GEMCITABINE FOR USE IN THE TREATMENT CANCER
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Page/Page column 18-19, (2012/04/23)
Phosphorodiamidate derivatives of e.g. gemcitabine are provided for use in treating cancer. In one embodiment, the two amidate motifs each comprises NR'R" where R' is H and R" is CR5R6CO2R7, where R6
