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Natural Product Research
Formerly Natural Product Letters
Volume 34, 2020 - Issue 16
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Research Articles

Synthesis and antitumor activity of camptothecin- 4β-triazolopodophyllotoxin conjugates

Cheng-Ting Zia Key Laboratory of Pu-er Tea Science, Ministry of Education, College of Science, Yunnan Agricultural University, Kunming, China; ;b State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, China; ;c Key Laboratory of Medicinal Chemistry for Nature Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming, China; Correspondence[email protected]
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,
Liu Yangb State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, China; View further author information
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Fa-Wu Dongb State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, China; View further author information
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Qing-Hua Kongb State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, China; View further author information
,
Zhong-Tao Dingc Key Laboratory of Medicinal Chemistry for Nature Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming, China; View further author information
,
Jun Zhoub State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, China; View further author information
,
Zi-Hua Jiangd Department of Chemistry, Lakehead University, Thunder Bay, ON, CanadaView further author information
&
Jiang-Miao Hub State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, China; View further author information
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Pages 2301-2309 | Received 08 Aug 2018, Accepted 15 Oct 2018, Published online: 12 Jan 2019
 
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Abstract

Two new compounds (9 and 10) having a camptothecin (CPT) analog conjugated to the 4β-azido-4-deoxypodophyllotixin analog by untilizing the copper-catalyzed azide-alkyne cycloadditon (CuAAC) reaction, and were evaluated for their cytotoxicity against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480) using the MTT (3-(4,5-dimethyl-thiahiazo-2-yl)-2,5-diphenyltetrazolium bromide) assay. Two novel conjugates shown weak cytotoxicity, compound 10 showed highly potent against HL-60 cell line tested, with IC50 value 17.69 ± 0.19 μM. This compound suggested its potential as anticancer agents for further development.

Disclosure statement

The authors declare no conflict of interest.

Additional information

Funding

This work was financially supported by Yunnan provincial science and technology department (2015HB093 and 2015FB168) and the National Key Research and Development Program of China (2017YFD0201402).

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