Synthesis and antitumor activity of novel ribonucleosides with C-5 OH replaced by a diaminopyrimidinyl group |
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| Authors: | Wang Kerang Wu Ling Qin Zhanbin Yan Xinhao Li Xiaoliu Chen Hua Zhang Pingzhu Zhang Jinchao |
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| Affiliation: | a Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding 071002, China
b State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China |
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| Abstract: | A series of novel ribonucleosides with C-5 OH replaced by a diaminopyrimidinyl group were synthesized by successively nucleophilic substitutions of 5′-deoxy-5′-amino-ribonucleosides with 2,4-dichloropyrimidine and then with various fatty amines under microwave irradiation. Their anticancer activities in vitro were preliminarily evaluated. Compounds 7a and 8a only exhibited anticancer activity against A549 cell line with the IC50 values of 10.73 and 10.99 μM, respectively. In addition, 7h and 8h showed potent activities against both A549 and Hela cell lines with the IC50 values of 12.71, 8.55 and 8.44, 5.55 μM, respectively. |
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| Keywords: | Ribonucleoside Pyrimidine Fatty amine Anticancer Nucleophilic substitution |
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