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Symmetrical Diamidates as a Class of Phosphate Prodrugs to Deliver the 5'-Monophosphate Forms of Anticancer Nucleoside Analogues.
- Source :
-
ChemMedChem [ChemMedChem] 2018 Nov 06; Vol. 13 (21), pp. 2305-2316. - Publication Year :
- 2018
-
Abstract
- 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.<br /> (© 2018 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)
- Subjects :
- Animals
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Cathepsin A chemistry
Cell Line, Tumor
Enzyme Assays
Humans
Mice
Molecular Structure
Organophosphorus Compounds chemical synthesis
Organophosphorus Compounds chemistry
Prodrugs chemical synthesis
Prodrugs chemistry
Purine Nucleosides chemical synthesis
Purine Nucleosides chemistry
Pyrimidine Nucleosides chemical synthesis
Pyrimidine Nucleosides chemistry
Antineoplastic Agents pharmacology
Organophosphorus Compounds pharmacology
Prodrugs pharmacology
Purine Nucleosides pharmacology
Pyrimidine Nucleosides pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1860-7187
- Volume :
- 13
- Issue :
- 21
- Database :
- MEDLINE
- Journal :
- ChemMedChem
- Publication Type :
- Academic Journal
- Accession number :
- 30199147
- Full Text :
- https://doi.org/10.1002/cmdc.201800504