title: Synthesis and Evaluation of New Podophyllotoxin Derivatives with in Vitro Anticancer Activity.
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-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.
authors.affiliation: Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China. cheng1083@163.com.
authors.forename: Wei-Hua
authors.initials: WH
authors.lastname: Cheng
authors.affiliation: Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China. shanghai0503@163.com.
authors.forename: Hai
authors.initials: H
authors.lastname: Shang
authors.affiliation: Pharmacognosy Division, Medical College of Chinese People's Armed Police Force, Tianjin 300162, China. anthritynika@163.com.
authors.forename: Cong
authors.initials: C
authors.lastname: Niu
authors.affiliation: Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin 300070, China. zhanghengxb@163.com.
authors.forename: Zhong-Heng
authors.initials: ZH
authors.lastname: Zhang
authors.affiliation: Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin 300070, China. 13920122174@163.com.
authors.forename: Li-Ming
authors.initials: LM
authors.lastname: Zhang
authors.affiliation: Pharmacognosy Division, Medical College of Chinese People's Armed Police Force, Tianjin 300162, China. anthritynika@163.com.|Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin 300070, China. anthritynika@163.com.
authors.forename: Hong
authors.initials: H
authors.lastname: Chen
authors.affiliation: Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China. zmzou@implad.ac.cn.
authors.forename: Zhong-Mei
authors.initials: ZM
authors.lastname: Zou
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D066298:In Vitro Techniques; D011034:Podophyllotoxin / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D011034:Podophyllotoxin
keywords: MDR; antitumor activity; podophyllotoxin; synthesized