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Synthesis, characterization and biological studies of diosgenyl analogues.

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机构： [1]Institute for Nanobiomedical Technology and Membrane Biology, and Laboratory of Ethnopharmacology, Regenerative Medicine Research Center, West China Hospital/West China Medical School, Sichuan University, Chengdu 610041, China

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关键词： Diosgenin-salicylate Asprin Amino acid Anti-tumor Anti-inflammatory

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A series of optical amino acid diosgenyl esters and diosgenyl salicylate conjugates were designed and synthesized to develop new anticancer and anti-inflammatory agents. The analogue 9c that contains an 6-aminohexanoic acid residue at C-3 of diosgenin exhibits higher potency against all three tumor cell lines with IC(50) values ranging from 4.7 μM in C26 cells to 14.6 μM in Hep G2 cells. In addition, seven of newly synthesized compounds significantly inhibit xylene-induced ear edema and exhibit comparable or better anti-inflammatory activities than those of diosgenin and aspirin. Furthermore, preliminary structure-activity relationship studies demonstrate that diosgenyl salicylate conjugates have stronger anti-inflammatory activities than amino acid diosgenyl esters. Copyright © 2012 Elsevier Ltd. All rights reserved.

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出版当年[2012]版：

大类 | 3 区医学

小类 | 3 区药物化学 3 区有机化学

最新[2023]版：

大类 | 4 区医学

小类 | 2 区有机化学 4 区药物化学

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第一作者机构： [1]Institute for Nanobiomedical Technology and Membrane Biology, and Laboratory of Ethnopharmacology, Regenerative Medicine Research Center, West China Hospital/West China Medical School, Sichuan University, Chengdu 610041, China

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