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Synthesis and Cytotoxic Activity of Novel C-23-Modified Asiatic Acid Derivatives

文献类型：期刊论文

作者Lu, Yi-hong1,2; Chen, Ming-cang1; Liu, Fang1,2; Xu, Zhou1; Tian, Xiao-ting1,2; Xie, Yang1; Huang, Cheng-gang1,2
刊名MOLECULES
出版日期2020-08-01
卷号25期号:16页码:20
关键词asiatic acid modification at C-23 intramolecular hydrogen bonding cytotoxic activity
DOI10.3390/molecules25163709
通讯作者Xie, Yang(sunshine_xie@163.com) ; Huang, Cheng-gang(cghsimm@126.com)
英文摘要We selectively oxidized the C-23 hydroxyl group in an asiatic acid (AA) derivative and then, for the first time with AA, modification of the C-23 carboxyl group was conducted to synthesize a series of new AA derivatives. The evaluation of their cytotoxic activities against two human cancer cell lines (SKOV-3 and HCT116) using the MTT assay in vitro revealed a distinctive structure activity relationship (SAR) associated with the intramolecular hydrogen bonding of the amide moiety at C-23. According to the established SAR, the cytotoxic activities of four promising compounds were then evaluated against MCF-7, A549, A2780, HepG2 and HL-60 cancer cell lines. Compound10had the best cytotoxic activity among all tested derivatives in the HL-60 cell line, giving IC50= 0.47 mu M, while showing no cytotoxic effect against human normal cells (HUVEC).
资助项目National Science and Technology Major Project of the Ministry of Science and Technology of China[2019ZX09201001-001-008] ; Youth Innovation Promotion Association of Chinese Academy of Sciences[2019280] ; National Natural Science Foundation of China for Young Scientists[81803828] ; China Postdoctoral Science Foundation[2018M642123]
WOS研究方向Biochemistry & Molecular Biology ; Chemistry
语种英语
WOS记录号WOS:000578804400001
出版者MDPI
源URL[http://119.78.100.183/handle/2S10ELR8/291430]  
专题中国科学院上海药物研究所
通讯作者Xie, Yang; Huang, Cheng-gang
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, 501 Haike Rd, Shanghai 201203, Peoples R China
2.Univ Chinese Acad Sci, Sch Pharm, 19A Yuquan Rd, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714		 Lu, Yi-hong,Chen, Ming-cang,Liu, Fang,et al. Synthesis and Cytotoxic Activity of Novel C-23-Modified Asiatic Acid Derivatives[J]. MOLECULES,2020,25(16):20.
APA Lu, Yi-hong.,Chen, Ming-cang.,Liu, Fang.,Xu, Zhou.,Tian, Xiao-ting.,...&Huang, Cheng-gang.(2020).Synthesis and Cytotoxic Activity of Novel C-23-Modified Asiatic Acid Derivatives.MOLECULES,25(16),20.
MLA Lu, Yi-hong,et al."Synthesis and Cytotoxic Activity of Novel C-23-Modified Asiatic Acid Derivatives".MOLECULES 25.16(2020):20.

入库方式： OAI收割

来源：上海药物研究所

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