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

Research output: Contribution to journal › Article › peer-review

34 Citations (Scopus)

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.

Original language	English
Pages (from-to)	615-627
Number of pages	13
Journal	European Journal of Medicinal Chemistry
Volume	103
DOIs	https://doi.org/10.1016/j.ejmech.2014.09.050
Publication status	Published - Oct 20 2015

Keywords

Azathioxanthones
Cytostatic and cytotoxic activities
MTT assay
NCI-60 human tumor cell lines
Topoisomerase assays

ASJC Scopus subject areas

Pharmacology
Drug Discovery
Organic Chemistry

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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.",

keywords = "Azathioxanthones, Cytostatic and cytotoxic activities, MTT assay, NCI-60 human tumor cell lines, Topoisomerase assays",

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 - Chen, Tsung Chih

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 - Cytostatic and cytotoxic activities

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

Abstract

Keywords

ASJC Scopus subject areas

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