文献类型： 外文期刊
作者： Xu, Tingting 2 ; Shi, Liqiao 1 ; Zhang, Yani 1 ; Wang, Kaimei 1 ; Yang, Ziwen 1 ; Ke, Shaoyong 1 ;
作者机构： 1.Hubei Acad Agr Sci, Hubei Biopesticide Engn Res Ctr, Natl Biopesticide Engn Res Ctr, Wuhan 430064, Hubei, Peoples R China
2.Wuhan Univ, Coll Life Sci, Wuhan 430072, Hubei, Peoples R China
关键词： Marine alkaloid; Pityriacitrin; Analogues; Synthesis; Biological evaluation; SARs
期刊名称：EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY （ 影响因子：6.514； 五年影响因子：6.099 ）
ISSN： 0223-5234
年卷期： 2019 年 168 卷
页码：
收录情况： SCI
摘要： Pityriacitrin is a marine alkaloid with typical beta-carboline scaffold, and which has been proven to exhibit diverse biological functions. During the course of our research for highly active compounds from natural products, the pityriacitrin have also been isolated and identified from a Chinese Burkholderia sp. NBF227. So, in order to explore the potential functional molecules, a series of beta-carboline analogues derived from pityriacitrin were designed and synthesized, and their in vitro cytotoxic activities against SGC-7901, A875, HepG2, and MARC145 cell lines were evaluated. The results demonstrated that some of these beta-carboline derivatives exhibited moderate to good cytotoxic activities, especially, compound 9o with a special sulfonyl group presented the highest inhibitory activities against all tested cell lines with the IC50 values of 6.82 +/- 0.98, 8.43 +/- 1.93, 7.69 +/- 2.17, 7.19 +/- 1.43 mu M, respectively, which might be used as lead compound for discovery of novel cytotoxic agents. (C) 2019 Elsevier Masson SAS. All rights reserved.
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