Cytotoxicity and in-vivo tolerance of FdUMP[10]: a novel pro-drug of the TS inhibitory nucleotide FdUMP.
The cytotoxicity of the 10mer ODN FdUMP[10] towards human colorectal tumor cells was evaluated using a clonogenic assay. FdUMP[10] was more than 100-fold more active than 5-FU at inhibiting colony formation of H630 cells. FdUMP[10] was also evaluated for cytotoxicity in the NCI 60 cell line screen, and showed markedly improved activity relative to 5-FU against numerous tumor cell lines. The in-vivo tolerance of FdUMP[10] is more than three-fold greater per mole fluorinated pyrimidine, than 5-FU.
Gmeiner
W H
WH
Eppley Institute, University of Nebraska Medical Center, Omaha 68198-6805, USA.
Skradis
A
A
Pon
R T
RT
Liu
J
J
D000970:Antineoplastic Agents / Q000494:pharmacology*; D002460:Cell Line; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000494:pharmacology; D005468:Fluorodeoxyuridylate / Q000494:pharmacology*; D006801:Humans; D011355:Prodrugs / Q000494:pharmacology*; D013940:Thymidylate Synthase / Q000037:antagonists & inhibitors*
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011355:Prodrugs; D005468:Fluorodeoxyuridylate; D013940:Thymidylate Synthase