Synthesis and biological evaluation of acylated oligorhamnoside derivatives structurally related to mezzettiaside-6 with cytotoxic activity
文献类型： 外文期刊
作者： Song, Gaopeng 1 ; Li, Sumei 3 ; Lei, Zhiwei 4 ; Li, Yibin 1 ; Li, Junhua 1 ; Liao, Yixian 1 ; Cui, Zi-Ning 2 ;
作者机构： 1.South China Agr Univ, Coll Mat & Energy, Guangzhou 510642, Guangdong, Peoples R China
2.South China Agr Univ, Guangdong Prov Key Lab Microbial Signals & Dis Co, Integrat Microbiol Res Ctr, State Key Lab Conservat & Utilizat Subtrop Agrobi, Guangzhou 510642, Guangdong, Peoples R China
3.Jinan Univ, Sch Med, Dept Human Anat, Guangzhou 510632, Guangdong, Peoples R China
4.Guizhou Acad Agr Sci, Guizhou Tea Reasearch Inst, Guiyang 550006, Guizhou, Peoples R China
期刊名称：ORGANIC & BIOMOLECULAR CHEMISTRY （ 影响因子：3.876； 五年影响因子：3.397 ）
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收录情况： SCI
摘要： Two partially acylated oligorhamnoside derivatives 1 and 2 structurally related to the natural product mezzettiaside-6 were synthesized via a '2 + 1 + 1' convergent strategy. The bioassay results showed that the introduction of the acetyl groups to the 2-position of the terminal L-rhamnose was helpful to improve in vitro cytotoxicity. Compound 1 showed both extensive in vitro cytotoxicity in tumor cell lines and potential antimultidrug resistance capability. Preliminary mechanistic studies demonstrated that compound 1 could inhibit cell growth by inducing apoptosis, arresting cell cycle progression at the S phase in K562 cells.
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