Design of antitumor agents containing carbohydrate based on GLUT1, and evaluation of antiproliferative activity |
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| Authors: | Renshuai Zhang Lairong Song Bo Jiang Lijun Wang Ning Wu Shuju Guo Dayong Shi |
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| Affiliation: | 1. Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences, Qingdao, China;2. Laboratory for Marine Drugs and Bioproducts, Qingdao National Laboratory for Marine Science and Technology, Qingdao, China;3. University of Chinese Academy of Sciences, Beijing, China;4. Department of Neurosurgery, The Affiliated Hospital of Qingdao University, Qingdao, China |
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| Abstract: | A series of novel carbohydrate-modified antitumor compounds were designed based on glucose transporter 1 (GLUT1), and evaluated for their anticancer activities against four cancer cell lines. The ribose derivatives (compound 9 and 10) exhibited modest inhibitory activity. The compound 9 significantly inhibited the migration of A549 cell and induced A549 cell apoptosis in a concentration-dependent manner. Moreover, compound 9 blocked A549 cells at the G0/G1 phase. The cellular uptake studies suggested that ribose-modified compound 9 could be taken through GLUT1 in A549 cell line. |
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| Keywords: | Saccharide GLUT1 Drug design Anticancer Cell uptake HSKDHPYQNOGXNU-KRBRLDSNSA-N |
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