Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives

doi:10.1007/s13659-017-0124-z

Natural Products and Bioprospecting ›› 2017, Vol. 7 ›› Issue (2): 215-223.DOI: 10.1007/s13659-017-0124-z

Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives

Xiu-Juan Yin^1,2, Chang-An Geng^1,3, Xing-Long Chen^1,2, Chang-Li Sun¹, Tong-Hua Yang^1,3, Tian-Ze Li^1,3, Jun Zhou¹, Xue-Mei Zhang^1,3, Ji-Jun Chen^1,3

1. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China;
2. University of Chinese Academy of Sciences, Beijing 100049, China;
3. Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China

Received:2016-12-19 Revised:2017-03-12 Online:2018-02-06 Published:2017-04-24
Supported by:
This work was supported by the Hundred Talents Program of the Chinese Academy of Sciences (CAS),the Youth Innovation Promotion Association,CAS and the Program of Yunling Scholarship.

Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives

Xiu-Juan Yin^1,2, Chang-An Geng^1,3, Xing-Long Chen^1,2, Chang-Li Sun¹, Tong-Hua Yang^1,3, Tian-Ze Li^1,3, Jun Zhou¹, Xue-Mei Zhang^1,3, Ji-Jun Chen^1,3

1. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China;
2. University of Chinese Academy of Sciences, Beijing 100049, China;
3. Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China

通讯作者: Ji-Jun Chen,e-mail:chenjj@mail.kib.ac.cn
基金资助:
This work was supported by the Hundred Talents Program of the Chinese Academy of Sciences (CAS),the Youth Innovation Promotion Association,CAS and the Program of Yunling Scholarship.

Abstract

Abstract: Sixteen tropinone derivatives were prepared,and their antitumor activities against five human cancer cells (HL- 60,A-549,SMMC-7721,MCF-7 and SW480) were evaluated with MTS[3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxy methoxyphenyl)-2-(4-sulfopheny)-2H-tetrazolium]assay.Most of the derivatives exhibited better activities compared with tropinone at the concentration of 40 lM.Particularly,derivative 6 showed significant activities with IC₅₀ values of 3.39, 13.59,6.65,13.09 and 12.38 μM respectively against HL-60,A-549,SMMC-7721,MCF-7 and SW480 cells,which suggested more potent activities than that of cis-dichlorodiamineplatinum (DDP).

摘要： Sixteen tropinone derivatives were prepared,and their antitumor activities against five human cancer cells (HL- 60,A-549,SMMC-7721,MCF-7 and SW480) were evaluated with MTS[3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxy methoxyphenyl)-2-(4-sulfopheny)-2H-tetrazolium]assay.Most of the derivatives exhibited better activities compared with tropinone at the concentration of 40 lM.Particularly,derivative 6 showed significant activities with IC₅₀ values of 3.39, 13.59,6.65,13.09 and 12.38 μM respectively against HL-60,A-549,SMMC-7721,MCF-7 and SW480 cells,which suggested more potent activities than that of cis-dichlorodiamineplatinum (DDP).

Xiu-Juan Yin, Chang-An Geng, Xing-Long Chen, Chang-Li Sun, Tong-Hua Yang, Tian-Ze Li, Jun Zhou, Xue-Mei Zhang, Ji-Jun Chen. Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives[J]. Natural Products and Bioprospecting, 2017, 7(2): 215-223.

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Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives

Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives

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