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Molecules 2015, 20(7), 12266-12279;

Synthesis and Evaluation of New Podophyllotoxin Derivatives with in Vitro Anticancer Activity

Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China
Pharmacognosy Division, Medical College of Chinese People's Armed Police Force, Tianjin 300162, China
Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin 300070, China
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 28 April 2015 / Revised: 28 June 2015 / Accepted: 29 June 2015 / Published: 6 July 2015
(This article belongs to the Section Medicinal Chemistry)
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A series of novel podophyllotoxin derivatives were designed and synthesized. The cytotoxic activities of these compounds were tested against three tumor cell lines (HeLa, K562, and K562/A02). Most of the derivatives (IC50 = 1–20 μM) were found to have stronger cell growth inhibitory activity than positive control etoposide. Among them, 4β-N-[(E)-(5-((4-(4-nitrophenyl)-piperazin-1-yl)methyl)furan-2-yl)prop-2-en-1-amine]-4-desoxy-podophyllotoxin (9l) demonstrated significant inhibitory activity against HeLa, K562, and K562/A02 cell lines with IC50 values of 7.93, 6.42, 6.89 μM, respectively. View Full-Text
Keywords: podophyllotoxin; MDR; synthesized; antitumor activity podophyllotoxin; MDR; synthesized; antitumor activity

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Cheng, W.-H.; Shang, H.; Niu, C.; Zhang, Z.-H.; Zhang, L.-M.; Chen, H.; Zou, Z.-M. Synthesis and Evaluation of New Podophyllotoxin Derivatives with in Vitro Anticancer Activity. Molecules 2015, 20, 12266-12279.

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