Structure-based hybridization, synthesis and biological evaluation of novel tetracyclic heterocyclic azathioxanthone analogues as potential antitumor agents

Tsung Chih Chen; Chia Lun Wu; Chia Chung Lee; Chun Liang Chen; Dah Shyong Yu; Hsu Shan Huang

doi:10.1016/j.ejmech.2014.09.050

Structure-based hybridization, synthesis and biological evaluation of novel tetracyclic heterocyclic azathioxanthone analogues as potential antitumor agents

Tsung Chih Chen
, Chia Lun Wu
, Chia Chung Lee
, Chun Liang Chen
, Dah Shyong Yu
, Hsu Shan Huang

研究成果: 雜誌貢獻 › 文章 › 同行評審

35 引文斯高帕斯（Scopus）

摘要

A series of tetracyclic heterocyclic azathioxanthones were synthesized and evaluated for cell proliferations, topoisomerase inhibitions, and NCI-60 cell panel assay, respectively. Compounds 5, 7, 8, 16, and 19 were selected for topoisomerase assay after MTT assay. 7 not only showed cytotoxic effect (IC50 Combining double low line 2.84 ± 0.64 μM) in PC-3 cells but also revealed topoisomerases inhibition with IC50 (10-25 μM) and increased apoptotic cleavage of PARP and caspase 3 activity. The overall of novel azathioxanthones with different cytostatic and cytotoxic activities should be further developed as new potential candidates for anticancer drugs.

原文	英語
頁（從 - 到）	615-627
頁數	13
期刊	European Journal of Medicinal Chemistry
卷	103
DOIs	https://doi.org/10.1016/j.ejmech.2014.09.050
出版狀態	已發佈 - 10月 20 2015

ASJC Scopus subject areas

藥理
藥物發現
有機化學

UN SDG

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10.1016/j.ejmech.2014.09.050

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title = "Structure-based hybridization, synthesis and biological evaluation of novel tetracyclic heterocyclic azathioxanthone analogues as potential antitumor agents",

abstract = "A series of tetracyclic heterocyclic azathioxanthones were synthesized and evaluated for cell proliferations, topoisomerase inhibitions, and NCI-60 cell panel assay, respectively. Compounds 5, 7, 8, 16, and 19 were selected for topoisomerase assay after MTT assay. 7 not only showed cytotoxic effect (IC50 Combining double low line 2.84 ± 0.64 μM) in PC-3 cells but also revealed topoisomerases inhibition with IC50 (10-25 μM) and increased apoptotic cleavage of PARP and caspase 3 activity. The overall of novel azathioxanthones with different cytostatic and cytotoxic activities should be further developed as new potential candidates for anticancer drugs.",

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author = "Chen, \{Tsung Chih\} and Wu, \{Chia Lun\} and Lee, \{Chia Chung\} and Chen, \{Chun Liang\} and Yu, \{Dah Shyong\} and Huang, \{Hsu Shan\}",

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AU - Wu, Chia Lun

AU - Lee, Chia Chung

AU - Chen, Chun Liang

AU - Yu, Dah Shyong

AU - Huang, Hsu Shan

PY - 2015/10/20

Y1 - 2015/10/20

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KW - Azathioxanthones

KW - Cytostatic and cytotoxic activities

KW - MTT assay

KW - NCI-60 human tumor cell lines

KW - Topoisomerase assays

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Structure-based hybridization, synthesis and biological evaluation of novel tetracyclic heterocyclic azathioxanthone analogues as potential antitumor agents

摘要

ASJC Scopus subject areas

UN SDG

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