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Journal of Asian Natural Products Research Volume 16, 2014 - Issue 5
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Articles

Synthesis and biological evaluation of novel podophyllotoxin analogs as antitumor agents

Zhong-Heng ZhangTianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin300070, China;Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazard, Department of Pharmacognosy, Logistics University of Chinese People's Armed Police Forces, Tianjin300162, China
,
Li-Ming ZhangTianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin300070, China;Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazard, Department of Pharmacognosy, Logistics University of Chinese People's Armed Police Forces, Tianjin300162, China
,
Gang LuoTianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin300070, China
,
Shi ZhangTianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazard, Department of Pharmacognosy, Logistics University of Chinese People's Armed Police Forces, Tianjin300162, China
,
Hong ChenTianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin300070, China;Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazard, Department of Pharmacognosy, Logistics University of Chinese People's Armed Police Forces, Tianjin300162, ChinaCorrespondence[email protected] [email protected]
&
Jing ZhouTianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin300070, ChinaCorrespondence[email protected] [email protected]
Pages 527-534 | Received 13 Nov 2013, Accepted 07 Apr 2014, Published online: 14 May 2014
 
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Abstract

A series of 4β N-indole-substituted podophyllotoxin derivatives were synthesized. Nine target compounds were evaluated against human cancer cell lines (HeLa, K562, and K562/A02) using MTT assay including three imine derivatives 8, 9, and 10in vitro. The result showed that the three compounds had higher antitumor activity than their reduced forms. Among them, compounds 8, 9, 11, and 16 were superior to the positive control VP-16.

Acknowledgments

This work was financially supported by the National Natural Science Foundation of China (No. 30873363), the Great Program of Science Foundation of Tianjin (No. 09ZCKFNC01200), and the Program of Science Foundation of Tianjin (No. 08JCYBJC070000).

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