Structure-based design, synthesis and biological evaluation of novel anthra[1,2-d]imidazole-6,11-dione homologues as potential antitumor agents

Tsung Chih Chen; Dah Shyong Yu; Kuo Feng Huang; Yung Chien Fu; Chia Chung Lee; Chun Liang Chen; Fong Chun Huang; Hsi Hsien Hsieh; Jing Jer Lin; Hsu Shan Huang

doi:10.1016/j.ejmech.2013.06.058

Structure-based design, synthesis and biological evaluation of novel anthra[1,2-d]imidazole-6,11-dione homologues as potential antitumor agents

Tsung Chih Chen, Dah Shyong Yu, Kuo Feng Huang, Yung Chien Fu, Chia Chung Lee, Chun Liang Chen, Fong Chun Huang, Hsi Hsien Hsieh, Jing Jer Lin, Hsu Shan Huang

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

26 Citations (Scopus)

Abstract

By using fragment-based design strategies, a series of 2-thio-substituted anthra[1,2-d]imidazole-6,11-diones were synthesized and evaluated for hTERT repressing activities, cell proliferations, and NCI 60-cell panel assay. Compounds 2, 3, 4, 11, 15 and 35 were selected by the NCI and 3, 4, 11 and 15 represent the GI₅₀, TGI and LC₅₀, respectively. Among them, all were moderate selectivity toward leukemia cancer except for 4 exhibited distinctive selectivity of CNS and renal cancer with 7.403 and 6.475. The overall of test compounds exhibited different cytostatic and cytotoxic activities for further developing potential application as anticancer drugs.

Original language	English
Pages (from-to)	278-293
Number of pages	16
Journal	European Journal of Medicinal Chemistry
Volume	69
DOIs	https://doi.org/10.1016/j.ejmech.2013.06.058
Publication status	Published - 2013
Externally published	Yes

Keywords

Anthra 12-dimidazole-611-dione
Cytostatic and cytotoxic activities
NCI 60-cell panel assay
Selectivity ratio

ASJC Scopus subject areas

Drug Discovery
Organic Chemistry
Pharmacology

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.ejmech.2013.06.058

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Chen, T. C., Yu, D. S., Huang, K. F., Fu, Y. C., Lee, C. C., Chen, C. L., Huang, F. C., Hsieh, H. H., Lin, J. J., & Huang, H. S. (2013). Structure-based design, synthesis and biological evaluation of novel anthra[1,2-d]imidazole-6,11-dione homologues as potential antitumor agents. European Journal of Medicinal Chemistry, 69, 278-293. https://doi.org/10.1016/j.ejmech.2013.06.058

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title = "Structure-based design, synthesis and biological evaluation of novel anthra[1,2-d]imidazole-6,11-dione homologues as potential antitumor agents",

abstract = "By using fragment-based design strategies, a series of 2-thio-substituted anthra[1,2-d]imidazole-6,11-diones were synthesized and evaluated for hTERT repressing activities, cell proliferations, and NCI 60-cell panel assay. Compounds 2, 3, 4, 11, 15 and 35 were selected by the NCI and 3, 4, 11 and 15 represent the GI50, TGI and LC50, respectively. Among them, all were moderate selectivity toward leukemia cancer except for 4 exhibited distinctive selectivity of CNS and renal cancer with 7.403 and 6.475. The overall of test compounds exhibited different cytostatic and cytotoxic activities for further developing potential application as anticancer drugs.",

keywords = "Anthra 12-dimidazole-611-dione, Cytostatic and cytotoxic activities, NCI 60-cell panel assay, Selectivity ratio",

author = "Chen, {Tsung Chih} and Yu, {Dah Shyong} and Huang, {Kuo Feng} and Fu, {Yung Chien} and Lee, {Chia Chung} and Chen, {Chun Liang} and Huang, {Fong Chun} and Hsieh, {Hsi Hsien} and Lin, {Jing Jer} and Huang, {Hsu Shan}",

year = "2013",

doi = "10.1016/j.ejmech.2013.06.058",

language = "English",

volume = "69",

pages = "278--293",

journal = "European Journal of Medicinal Chemistry",

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T1 - Structure-based design, synthesis and biological evaluation of novel anthra[1,2-d]imidazole-6,11-dione homologues as potential antitumor agents

AU - Chen, Tsung Chih

AU - Yu, Dah Shyong

AU - Huang, Kuo Feng

AU - Fu, Yung Chien

AU - Lee, Chia Chung

AU - Chen, Chun Liang

AU - Huang, Fong Chun

AU - Hsieh, Hsi Hsien

AU - Lin, Jing Jer

AU - Huang, Hsu Shan

PY - 2013

Y1 - 2013

N2 - By using fragment-based design strategies, a series of 2-thio-substituted anthra[1,2-d]imidazole-6,11-diones were synthesized and evaluated for hTERT repressing activities, cell proliferations, and NCI 60-cell panel assay. Compounds 2, 3, 4, 11, 15 and 35 were selected by the NCI and 3, 4, 11 and 15 represent the GI50, TGI and LC50, respectively. Among them, all were moderate selectivity toward leukemia cancer except for 4 exhibited distinctive selectivity of CNS and renal cancer with 7.403 and 6.475. The overall of test compounds exhibited different cytostatic and cytotoxic activities for further developing potential application as anticancer drugs.

AB - By using fragment-based design strategies, a series of 2-thio-substituted anthra[1,2-d]imidazole-6,11-diones were synthesized and evaluated for hTERT repressing activities, cell proliferations, and NCI 60-cell panel assay. Compounds 2, 3, 4, 11, 15 and 35 were selected by the NCI and 3, 4, 11 and 15 represent the GI50, TGI and LC50, respectively. Among them, all were moderate selectivity toward leukemia cancer except for 4 exhibited distinctive selectivity of CNS and renal cancer with 7.403 and 6.475. The overall of test compounds exhibited different cytostatic and cytotoxic activities for further developing potential application as anticancer drugs.

KW - Anthra 12-dimidazole-611-dione

KW - Cytostatic and cytotoxic activities

KW - NCI 60-cell panel assay

KW - Selectivity ratio

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SN - 0223-5234

VL - 69

SP - 278

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JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

Structure-based design, synthesis and biological evaluation of novel anthra[1,2-d]imidazole-6,11-dione homologues as potential antitumor agents

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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