Semisynthesis and in vitro cytotoxic evaluation of new analogues of 1-O-acetylbritannilactone, a sesquiterpene from Inula britannica
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- 作者：Shuai Dong ; Jiang-Jiang Tang ; tangjiang11@nwsuaf.edu.cn" class="auth_mail ; Cheng-Chen Zhang ; Jun-Mian Tian ; Jun-Tao Guo ; Qiang Zhang ; He Li ; Jin-Ming Gao ; jinminggao@nwsuaf.edu.cn" class="auth_mail
- 关键词：1-O-Acetylbritannilactone sesquiterpene ; Cytotoxic activity ; Structure&ndash ; activity relationship
- 刊名：European Journal of Medicinal Chemistry
- 出版年：10 June 2014
- 年：2014
- 卷：80
- 期：Complete
- 页码：71-82
- 全文大小：1615 K
文摘
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Absolute configuration of ABL was confirmed by X-ray diffraction analysis.
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A series of novel 6-OH modified and C13 arylation analogues was synthesized.
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6-OH esterified compounds showed potent cytotoxic activities.
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Compound 14 displayed remarkable cytotoxic activity, comparable to etoposide.
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14 triggered apoptosis and cell cycle arrest at G2/M phase in HCT116 cells.