Design, synthesis, and antitumor activity of bile acid-polyamine-nucleoside conjugates.
A series of bile acid-polyamine amides conjugated with 3'-azido-3'-deoxythymidine (AZT) as potential antitumor prodrugs in the form of phosphoramidates were synthesized in good yields and their antitumor activities were assayed against two human cancer cells in vitro: cervix cancer HeLa cells and renal cancer 7860 cells. The improved antitumor activity probably derived from the enhanced delivery efficiency of AZT due to bile acid-polyamine conjugates.
Wu
Dimao
D
Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Ministry of Education, Department of Chemistry, Tsinghua University, Beijing 100084, PR China.
Ji
Sanhao
S
Wu
Yan
Y
Ju
Yong
Y
Zhao
Yufen
Y
D000577:Amides / Q000737:chemistry; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001647:Bile Acids and Salts / Q000737:chemistry*; D045744:Cell Line, Tumor; D016503:Drug Delivery Systems; D015195:Drug Design; D006367:HeLa Cells; D006801:Humans; D009705:Nucleosides / Q000737:chemistry; D010756:Phosphoric Acids / Q000737:chemistry; D011073:Polyamines / Q000737:chemistry*; D011355:Prodrugs / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015215:Zidovudine / Q000737:chemistry / Q000494:pharmacology*
D000577:Amides; D000970:Antineoplastic Agents; D001647:Bile Acids and Salts; D009705:Nucleosides; D010756:Phosphoric Acids; D011073:Polyamines; D011355:Prodrugs; D015215:Zidovudine; C011067:phosphoramidic acid