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

Molecules

Wei-Hua Cheng²  Hai Shang²  Cong Niu¹  Zhong-Heng Zhang³  Li-Ming Zhang³  Hong Chen¹  Zhong-Mei Zou² 

[1] Pharmacognosy Division, Medical College of Chinese People’s Armed Police Force, Tianjin 300162, China; E-Mail:;Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China; E-Mails:;Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin 300070, China; E-Mails:

关键词: podophyllotoxin;    MDR;    synthesized;    antitumor activity;   

DOI  :  10.3390/molecules200712266

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.