Design, synthesis, and antitumor activity of bile acid-polyamine-nucleoside conjugates |
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| Authors: | Wu Dimao Ji Sanhao Wu Yan Ju Yong Zhao Yufen |
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| Affiliation: | Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Ministry of Education, Department of Chemistry, Tsinghua University, Beijing 100084, PR China. |
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| Abstract: | 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. |
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