Synthesis, antiproliferative activities and telomerase inhibition evaluation of novel asymmetrical 1,2-disubstituted amidoanthraquinone derivatives

Chia Chung Lee; Kuo Feng Huang; Pen Yuan Lin; Fong Chun Huang; Chun Liang Chen; Tsung Chih Chen; Jih Hwa Guh; Jing Jer Lin; Hsu Shan Huang

doi:10.1016/j.ejmech.2011.10.059

Synthesis, antiproliferative activities and telomerase inhibition evaluation of novel asymmetrical 1,2-disubstituted amidoanthraquinone derivatives

Chia Chung Lee, Kuo Feng Huang, Pen Yuan Lin, Fong Chun Huang, Chun Liang Chen, Tsung Chih Chen, Jih Hwa Guh, Jing Jer Lin, Hsu Shan Huang

研究成果: 雜誌貢獻 › 文章 › 同行評審

25 引文斯高帕斯（Scopus）

摘要

A series of diversely asymmetrical mono- or disubstituted 1,2-diamidoanthraquinone derivatives were synthesized and evaluated for drug-induced cytotoxicity by SRB assay, telomerase inhibitory activity by TRAP assay, and hTERT expression by SEAP assay. Interestingly, compounds 4, 11, 21, 32 and 36 exhibited selective potent antiproliferative activities by NCI with IC 50 values in the micromolar range. Of these, only compound 8 showed an IC 50 value of 0.95 μM against PC-3 cell lines (human prostate cancer) by SRB assay. All the synthesized compounds exhibited a poor or modest telomerase inhibitory activity by TRAP assay suggesting another mode of action for these compounds. Compound 11 showed broad inhibition against different types of cancer cell lines in the micromolar and submicromolar range.

原文	英語
頁（從 - 到）	323-336
頁數	14
期刊	European Journal of Medicinal Chemistry
卷	47
發行號	1
DOIs	https://doi.org/10.1016/j.ejmech.2011.10.059
出版狀態	已發佈 - 1月 2012

ASJC Scopus subject areas

藥物發現
有機化學
藥理

UN SDG

此研究成果有助於以下永續發展目標

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10.1016/j.ejmech.2011.10.059

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Lee, C. C., Huang, K. F., Lin, P. Y., Huang, F. C., Chen, C. L., Chen, T. C., Guh, J. H., Lin, J. J., & Huang, H. S. (2012). Synthesis, antiproliferative activities and telomerase inhibition evaluation of novel asymmetrical 1,2-disubstituted amidoanthraquinone derivatives. European Journal of Medicinal Chemistry, 47(1), 323-336. https://doi.org/10.1016/j.ejmech.2011.10.059

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title = "Synthesis, antiproliferative activities and telomerase inhibition evaluation of novel asymmetrical 1,2-disubstituted amidoanthraquinone derivatives",

abstract = "A series of diversely asymmetrical mono- or disubstituted 1,2-diamidoanthraquinone derivatives were synthesized and evaluated for drug-induced cytotoxicity by SRB assay, telomerase inhibitory activity by TRAP assay, and hTERT expression by SEAP assay. Interestingly, compounds 4, 11, 21, 32 and 36 exhibited selective potent antiproliferative activities by NCI with IC 50 values in the micromolar range. Of these, only compound 8 showed an IC 50 value of 0.95 μM against PC-3 cell lines (human prostate cancer) by SRB assay. All the synthesized compounds exhibited a poor or modest telomerase inhibitory activity by TRAP assay suggesting another mode of action for these compounds. Compound 11 showed broad inhibition against different types of cancer cell lines in the micromolar and submicromolar range.",

keywords = "Anthraquinone, NCI 60-cell panel assay, Sulforhodamine B (SRB) assay, Telomerase activity, TRAP assay",

author = "Lee, {Chia Chung} and Huang, {Kuo Feng} and Lin, {Pen Yuan} and Huang, {Fong Chun} and Chen, {Chun Liang} and Chen, {Tsung Chih} and Guh, {Jih Hwa} and Lin, {Jing Jer} and Huang, {Hsu Shan}",

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AU - Lee, Chia Chung

AU - Huang, Kuo Feng

AU - Lin, Pen Yuan

AU - Huang, Fong Chun

AU - Chen, Chun Liang

AU - Chen, Tsung Chih

AU - Guh, Jih Hwa

AU - Lin, Jing Jer

AU - Huang, Hsu Shan

PY - 2012/1

Y1 - 2012/1

N2 - A series of diversely asymmetrical mono- or disubstituted 1,2-diamidoanthraquinone derivatives were synthesized and evaluated for drug-induced cytotoxicity by SRB assay, telomerase inhibitory activity by TRAP assay, and hTERT expression by SEAP assay. Interestingly, compounds 4, 11, 21, 32 and 36 exhibited selective potent antiproliferative activities by NCI with IC 50 values in the micromolar range. Of these, only compound 8 showed an IC 50 value of 0.95 μM against PC-3 cell lines (human prostate cancer) by SRB assay. All the synthesized compounds exhibited a poor or modest telomerase inhibitory activity by TRAP assay suggesting another mode of action for these compounds. Compound 11 showed broad inhibition against different types of cancer cell lines in the micromolar and submicromolar range.

AB - A series of diversely asymmetrical mono- or disubstituted 1,2-diamidoanthraquinone derivatives were synthesized and evaluated for drug-induced cytotoxicity by SRB assay, telomerase inhibitory activity by TRAP assay, and hTERT expression by SEAP assay. Interestingly, compounds 4, 11, 21, 32 and 36 exhibited selective potent antiproliferative activities by NCI with IC 50 values in the micromolar range. Of these, only compound 8 showed an IC 50 value of 0.95 μM against PC-3 cell lines (human prostate cancer) by SRB assay. All the synthesized compounds exhibited a poor or modest telomerase inhibitory activity by TRAP assay suggesting another mode of action for these compounds. Compound 11 showed broad inhibition against different types of cancer cell lines in the micromolar and submicromolar range.

KW - Anthraquinone

KW - NCI 60-cell panel assay

KW - Sulforhodamine B (SRB) assay

KW - Telomerase activity

KW - TRAP assay

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Synthesis, antiproliferative activities and telomerase inhibition evaluation of novel asymmetrical 1,2-disubstituted amidoanthraquinone derivatives

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ASJC Scopus subject areas

UN SDG

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