Naphthyl phosphoramidate derivatives of BVdU as potential anticancer agents: design, synthesis and biological evaluation.
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.
Congiatu
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C
Welsh School of Pharmacy, Cardiff University, Cardiff, UK. sphcc3@cf.ac.uk
McGuigan
C
C
Jiang
W G
WG
Davies
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G
Mason
M D
MD
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*
D000577:Amides; D000970:Antineoplastic Agents; D000998:Antiviral Agents; C421011:NB1011; D010756:Phosphoric Acids; C020235:brivudine; C011067:phosphoramidic acid; D001973:Bromodeoxyuridine