Novel nucleotide phosphonate analogues with potent antitumor activity.
We have identified several nucleotide phosphonates demonstrating in vitro antiproliferative activity in several human cancer cell lines with IC(50) values in the microM range. The synthesis as well as structure-activity relationship are described.
Bubenik
Monica
M
Shire BioChem Inc., 275 Armand-Frappier Blvd., Laval, Québec, Canada H7V 4A7. mbubenik@ca.shire.com
Rej
Rabindra
R
Nguyen-Ba
Nghe
N
Attardo
Giorgio
G
Ouellet
France
F
Chan
Laval
L
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D005663:Furans / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D009711:Nucleotides / Q000138:chemical synthesis* / Q000494:pharmacology*; D063065:Organophosphonates / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013936:Thymidine / Q000378:metabolism; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D005663:Furans; D009711:Nucleotides; D063065:Organophosphonates; C018674:tetrahydrofuran; D013936:Thymidine