Synthesis and cytotoxicity of novel fatty acid-nucleoside conjugates.
N(3)-Hydroxyethyltegafur (3) was synthesized in 91.0% yield under a new condition. A series of novel fatty acid esters of 3 were synthesized. These fatty acid-nucleoside conjugates have shown cytotoxicities against Ec9706 cells and A549 cells, and the structure activity relationship was discussed.
Zhang
Yun-Xiao
YX
Department of Chemistry, New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450052, PR China.
Dai
Gui-Fu
GF
Wang
Le
L
Tao
Jing-Chao
JC
D000964:Antimetabolites, Antineoplastic / Q000138:chemical synthesis* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D004952:Esters / Q000138:chemical synthesis / Q000494:pharmacology; D005227:Fatty Acids / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D009705:Nucleosides / Q000138:chemical synthesis* / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization; D013329:Structure-Activity Relationship; D005641:Tegafur / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology
D000964:Antimetabolites, Antineoplastic; D000970:Antineoplastic Agents; D004952:Esters; D005227:Fatty Acids; D009705:Nucleosides; D005641:Tegafur