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

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 (IC(50) = 1–20 μM) were found to have stronger cell growth inhibitory activity than...

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Detalles Bibliográficos
Autores principales: Cheng, Wei-Hua, Shang, Hai, Niu, Cong, Zhang, Zhong-Heng, Zhang, Li-Ming, Chen, Hong, Zou, Zhong-Mei
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2015
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6332074/
https://www.ncbi.nlm.nih.gov/pubmed/26154885
http://dx.doi.org/10.3390/molecules200712266
Descripción
Sumario: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 (IC(50) = 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 IC(50) values of 7.93, 6.42, 6.89 μM, respectively.

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