1H-NMR、13C-NMR、HR-MS確定其結(jié)構(gòu),其中17個衍生物首次得到。部分衍生物表現(xiàn)出良好的抗腫瘤活性,芐胺基團(tuán)對此類骨架化合物的結(jié)構(gòu)修飾能夠較好地提高其抗腫瘤活性。結(jié)論 部分衍生物表現(xiàn)出良好的抗腫瘤活性,特別對HepG2細(xì)胞活性有較大的提高,化合物12、22、23具有進(jìn)一步研究價值。;Objective To modify derivatives of 6 natural sesquiterpenoids from Hibiscus tiliaceus Linn., evaluate their in vitro antitumor activities, and reveal the structure-activity relationship. Methods A series of amines from H. tiliaceus were used to synthesize the gossypol Schiff base of the 6 sesquiterpenoids. Their antitumor activities in vitro were evaluated for HeLa, HepG2, and MCG-803 by MTT assay. Results Nineteen derivatives were synthesized, seventeen of which was reported for the first time, and their structures were characterized by 1H-NMR, 13C-NMR, and HR-MS. MTT assay showed some sesquiterpenoid derivatives exhibited good antitumor activity against HeLa, HepG2, and MCG-803 cell, and benzylamine modification could enhance antitumor activity of these sesquiterpenoid skeletons. Conclusion Some derivatives show promising antitumor activities, especially for the HepG2 cell lines, and compound 12, 22, and 23 are worth further studying."/>

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首頁 > 過刊瀏覽>2022年第37卷第3期 >2022,37(3):445-452. DOI:10.7501/j.issn.1674-5515.2022.03.001
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6種黃槿倍半萜類成分的衍生化改造和體外抗腫瘤活性研究

Modify and in vitro antitumor activity evaluation of six sesquiterpenoid components derivatives from Hibiscus tiliaceus

發(fā)布日期:2022-03-22