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孙冬宇, 龚景旭, 李序文, 韩冠英, 郭跃伟. Methyl Xestospongoate类似物的设计、合成和抗肿瘤活性[J]. 中国药科大学学报, 2018, 49(4): 413-421. DOI: 10.11665/j.issn.1000-5048.20180405
引用本文: 孙冬宇, 龚景旭, 李序文, 韩冠英, 郭跃伟. Methyl Xestospongoate类似物的设计、合成和抗肿瘤活性[J]. 中国药科大学学报, 2018, 49(4): 413-421. DOI: 10.11665/j.issn.1000-5048.20180405
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SUN Dongyu, GONG Jingxu, LI Xuwen, HAN Guanying, GUO Yuewei. Studies on methyl xestopongoate analogues:design, synthesis and antitumor activities[J]. Journal of China Pharmaceutical University, 2018, 49(4): 413-421. DOI: 10.11665/j.issn.1000-5048.20180405
Citation: SUN Dongyu, GONG Jingxu, LI Xuwen, HAN Guanying, GUO Yuewei. Studies on methyl xestopongoate analogues:design, synthesis and antitumor activities[J]. Journal of China Pharmaceutical University, 2018, 49(4): 413-421. DOI: 10.11665/j.issn.1000-5048.20180405
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Methyl Xestospongoate类似物的设计、合成和抗肿瘤活性

Studies on methyl xestopongoate analogues:design, synthesis and antitumor activities

    摘要
  • 摘要: 设计、合成了52个Methyl Xestospongoate类似物并初步研究了其抗肿瘤活性。以炔基甲酯和二炔为原料，经过Cadiot-Chodkiewitz偶联和Sonogashira偶联反应合成了52个Methyl Xestospongoate类似物 4(a~m) - 7( a ~ m )，并利用1H NMR、13C NMR和HREI-MS法确定其结构，采用CCK-8法测定了部分化合物的体外抗肿瘤活性。结果显示化合物 6k 对A549和P-388肿瘤细胞的增殖具有较强的抑制活性，其IC50分别为9.36和9.62 μmol/L。

     

    Abstract: Fifty-two methyl xestospongoate analogues were designed, synthesized and evaluated for the antiproliferative activity. Starting from alkynyl methyl ester and diyne, methyl xestospongoate analogues 4 ( a - m )- 7( a - m )were synthesized by Cadiot-Chodkiewitz coupling and Sonogashira coupling reactions. Their structures were identified by 1H NMR, 13C NMR and HREI-MS. The cytotoxic inhibiton activities in vitro of some compounds were evaluated against human cancer cells A549 and P-388 by a CCK-8 method. Among them, compound 6k exhibited potent cell growth inhibitory activity against A549 and P-388 cancer cells, with IC50 values of 9. 36 and 9. 62 μmol/L, respectively.

     

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