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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 ?M) were found to have stronger cell growth inhibitory activity than positive control etoposide. Among them, 4?-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 ?M, respectively.

SUBMITTER: Cheng WH

PROVIDER: S-EPMC6332074 | biostudies-literature | 2015 Jul

REPOSITORIES: biostudies-literature

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

Cheng Wei-Hua WH Shang Hai H Niu Cong C Zhang Zhong-Heng ZH Zhang Li-Ming LM Chen Hong H Zou Zhong-Mei ZM

Molecules (Basel, Switzerland) 20150706 7

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 ag ...[more]

PMID: 26154885

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