Synthesis and Evaluation of New Podophyllotoxin Derivatives with in Vitro Anticancer Activity
Wei-Hua Cheng,
Hai Shang,
Cong Niu,
Zhong-Heng Zhang,
Li-Ming Zhang,
Hong Chen,
Zhong-Mei Zou
Affiliations
Wei-Hua Cheng
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China
Hai Shang
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China
Cong Niu
Pharmacognosy Division, Medical College of Chinese People's Armed Police Force, Tianjin 300162, China
Zhong-Heng Zhang
Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin 300070, China
Li-Ming Zhang
Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin 300070, China
Hong Chen
Pharmacognosy Division, Medical College of Chinese People's Armed Police Force, Tianjin 300162, China
Zhong-Mei Zou
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China
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.
