title: Naphthyl phosphoramidate derivatives of BVdU as potential anticancer agents: design, synthesis and biological evaluation.
abstract: The phosphoramidate technology we have developed has been recently applied to BVdU, leading to NB1011 (NewBiotics Inc., California), a novel potential anticancer compound recently entered into phase 2 of the clinical trials for colon cancer. We report in this work a new series of derivatives containing naphthol as aryl masking group on the phosphate moiety, which has shown a significant increase in anticancer activity in preliminary biological evaluations.
authors.affiliation: Welsh School of Pharmacy, Cardiff University, Cardiff, UK. sphcc3@cf.ac.uk
authors.forename: C
authors.initials: C
authors.lastname: Congiatu
authors.forename: C
authors.initials: C
authors.lastname: McGuigan
authors.forename: W G
authors.initials: WG
authors.lastname: Jiang
authors.forename: G
authors.initials: G
authors.lastname: Davies
authors.forename: M D
authors.initials: MD
authors.lastname: Mason
mesh_terms: D000577:Amides / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000998:Antiviral Agents / Q000494:pharmacology; D001973:Bromodeoxyuridine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D045744:Cell Line, Tumor; D003110:Colonic Neoplasms / Q000188:drug therapy; D005260:Female; D006801:Humans; D008297:Male; D008956:Models, Chemical; D010756:Phosphoric Acids / Q000737:chemistry*
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D000998:Antiviral Agents; C421011:NB1011; D010756:Phosphoric Acids; C020235:brivudine; C011067:phosphoramidic acid; D001973:Bromodeoxyuridine