3-epi-Jaspine B类似物的合成和抗肿瘤活性评价  

Synthesis and Antitumor Evaluation of 3-epi-Jaspine B Analogues

作　　者：张恩[1] 王上[1] 焦伟伟[1] 王铭铭[1] 岳静飞 徐帅民 王亚娜[1] Horst-Dieter Ambrosi 刘宏民[1] 

机构地区：[1]郑州大学药学院,新药创制与药物安全性评价河南省协同创新中心,郑州450001 [2]AnalytiCon Discovery GmbH,Hermannswerder Haus 17,14473 Potsdam,Germany

出　　处：《有机化学》2017年第1期141-148,共8页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.U1204206);河南省教育厅(No.17A350004)资助项目~~

摘　　要：Jaspine B是从海绵中提取的具有显著肿瘤活性的天然产物.为了寻找活性更好,合成方法更简洁的抗肿瘤化合物,设计并合成了一系列3-epi-Jaspine B类似物,共16个化合物,所合成的化合物均未见文献报道.所有化合物都经过~1H NMR、^(13)C NMR和HRMS确定分子结构.对所合成的化合物用噻唑蓝(MTT)法对4种肿瘤细胞(B16-F10小鼠皮肤黑色素瘤细胞、A-549人肺癌细胞、MCF-7人乳腺癌细胞、PC-3人前列腺癌细胞)进行生物活性测试,部分化合物对肿瘤细胞有抑制作用,其中化合物8f和11对A-549人肺癌细胞具有较好的活性,其IC_(50)分别为(9.646±0.984)和(7.144±0.854)μg/m L.Jaspine B is a natural product with significant antitumor activity, which was isolated from the marine sponge Pachastrissa sp. In order to find new antitumor compounds with high efficiency and succinct synthetic methods, a series of 3-epi-jaspine B analogues were designed and synthesized. 16 compounds were synthesized and all of them were unknown in the literature. Their structures were determined by 1H NMR, 13C NMR and HRMS. The antitumor activity of these compounds against four tumor cell lines B16-F10, A-549, MCF-7 and PC-3 was assayed using thiazolyl blue（MTT） assay, and some compounds showed potent inhibitory effect on tumor cells. Compounds 8f and 11 were more potent against A-549 with IC_（50） of（9.646±0.984） and（7.144±0.854） μg/m L.

关 键 词：3-epi-jaspine B 抗肿瘤 硫化氢 类似物 

分 类 号：O629[理学—有机化学]