Synthesis and Evaluation of New Podophyllotoxin Derivatives with in Vitro Anticancer ActivityReport as inadecuate




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1

Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China

2

Pharmacognosy Division, Medical College of Chinese Peoples Armed Police Force, Tianjin 300162, China

3

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

Abstract 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-ylmethylfuran-2-ylprop-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





Author: Wei-Hua Cheng 1,†, Hai Shang 1,†, Cong Niu 2, Zhong-Heng Zhang 3, Li-Ming Zhang 3, Hong Chen 2,3 and Zhong-Mei Zou 1,*

Source: http://mdpi.com/



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