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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and antiproliferative evaluation of 23-hydroxybetulinic acid derivatives.
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Synthesis and antiproliferative evaluation of 23-hydroxybetulinic acid derivatives.

机译：23-羟基贝丁酸衍生物的合成和抗增殖评价。

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摘要

Based on structural modifications of the natural 23-hydroxybetulinic acid, a series of novel its derivatives had been synthesized. The new compounds were screened for in vitro antiproliferative activity against cancer cell lines HeLa, MCF-7, HepG2, B16 and A375 using doxorubicin as a reference. The vast majority of derivatives had exhibited potent tumor growth inhibitory activity than original compound. The derivatives 4, 5, 7, 20, 23, 26, 43 and 44 with IC50 values lower than 10 muM on all tested cell lines were regarded as the most promising compounds. The structure-activity relationships of 23-hydroxybetulinic acid derivatives were also discussed in the present investigations.
机译：基于对天然23-羟基贝丁酸的结构修饰，已合成了一系列新颖的衍生物。使用阿霉素作为参考，筛选了新化合物对癌细胞系HeLa，MCF-7，HepG2，B16和A375的体外抗增殖活性。绝大多数衍生物比原始化合物显示出有效的肿瘤生长抑制活性。在所有测试的细胞系上IC50值均低于10μM的衍生物4、5、7、20、23、26、43和44被认为是最有希望的化合物。在本研究中还讨论了23-羟基贝丁酸衍生物的构效关系。

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