Design, synthesis and evaluation of telomerase inhibitory, hTERT repressing, and anti-proliferation activities of symmetrical 1,8-disubstituted amidoanthraquinones

Chia Chung Lee; Kuo Feng Huang; Deh Ming Chang; Jung Jung Hsu; Fong Chun Huang; Kai Ning Shih; Chun Liang Chen; Tsung Chih Chen; Ruei Huei Chen; Jing Jer Lin; Hsu Shan Huang

doi:10.1016/j.ejmech.2012.01.044

Design, synthesis and evaluation of telomerase inhibitory, hTERT repressing, and anti-proliferation activities of symmetrical 1,8-disubstituted amidoanthraquinones

Chia Chung Lee, Kuo Feng Huang, Deh Ming Chang, Jung Jung Hsu, Fong Chun Huang, Kai Ning Shih, Chun Liang Chen, Tsung Chih Chen, Ruei Huei Chen, Jing Jer Lin, Hsu Shan Huang

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

22 Citations (Scopus)

Abstract

A series of symmetrical disubstituded 1,8-diamidoanthraquinones were synthesized and evaluated for anti-proliferation, telomerase inhibitory by TRAP assay, and hTERT expression by SEAP assay. All of the compounds tested, except for compounds 3a and 3s were selected by the NCI screening system. In addition, compounds 4e and 4k exhibited inhibitory effects on telomerase activity. Taken together, our findings indicated that the analysis of cytotoxicity and telomerase inhibition might provide information applicable for further developing potential telomerase targeting strategy.

Original language	English
Pages (from-to)	102-112
Number of pages	11
Journal	European Journal of Medicinal Chemistry
Volume	50
DOIs	https://doi.org/10.1016/j.ejmech.2012.01.044
Publication status	Published - Apr 2012
Externally published	Yes

Keywords

Amidoanthraquinones
NCI 60-cell panel assay
SEAP assay
TRAP assay
Telomerase
hTERT expression

ASJC Scopus subject areas

Drug Discovery
Pharmacology
Organic Chemistry

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10.1016/j.ejmech.2012.01.044

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Lee, C. C., Huang, K. F., Chang, D. M., Hsu, J. J., Huang, F. C., Shih, K. N., Chen, C. L., Chen, T. C., Chen, R. H., Lin, J. J., & Huang, H. S. (2012). Design, synthesis and evaluation of telomerase inhibitory, hTERT repressing, and anti-proliferation activities of symmetrical 1,8-disubstituted amidoanthraquinones. European Journal of Medicinal Chemistry, 50, 102-112. https://doi.org/10.1016/j.ejmech.2012.01.044

Lee, CC, Huang, KF, Chang, DM, Hsu, JJ, Huang, FC, Shih, KN, Chen, CL, Chen, TC, Chen, RH, Lin, JJ & Huang, HS 2012, 'Design, synthesis and evaluation of telomerase inhibitory, hTERT repressing, and anti-proliferation activities of symmetrical 1,8-disubstituted amidoanthraquinones', European Journal of Medicinal Chemistry, vol. 50, pp. 102-112. https://doi.org/10.1016/j.ejmech.2012.01.044

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title = "Design, synthesis and evaluation of telomerase inhibitory, hTERT repressing, and anti-proliferation activities of symmetrical 1,8-disubstituted amidoanthraquinones",

abstract = "A series of symmetrical disubstituded 1,8-diamidoanthraquinones were synthesized and evaluated for anti-proliferation, telomerase inhibitory by TRAP assay, and hTERT expression by SEAP assay. All of the compounds tested, except for compounds 3a and 3s were selected by the NCI screening system. In addition, compounds 4e and 4k exhibited inhibitory effects on telomerase activity. Taken together, our findings indicated that the analysis of cytotoxicity and telomerase inhibition might provide information applicable for further developing potential telomerase targeting strategy.",

keywords = "Amidoanthraquinones, NCI 60-cell panel assay, SEAP assay, TRAP assay, Telomerase, hTERT expression",

author = "Lee, {Chia Chung} and Huang, {Kuo Feng} and Chang, {Deh Ming} and Hsu, {Jung Jung} and Huang, {Fong Chun} and Shih, {Kai Ning} and Chen, {Chun Liang} and Chen, {Tsung Chih} and Chen, {Ruei Huei} and Lin, {Jing Jer} and Huang, {Hsu Shan}",

year = "2012",

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doi = "10.1016/j.ejmech.2012.01.044",

language = "English",

volume = "50",

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journal = "European Journal of Medicinal Chemistry",

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T1 - Design, synthesis and evaluation of telomerase inhibitory, hTERT repressing, and anti-proliferation activities of symmetrical 1,8-disubstituted amidoanthraquinones

AU - Lee, Chia Chung

AU - Huang, Kuo Feng

AU - Chang, Deh Ming

AU - Hsu, Jung Jung

AU - Huang, Fong Chun

AU - Shih, Kai Ning

AU - Chen, Chun Liang

AU - Chen, Tsung Chih

AU - Chen, Ruei Huei

AU - Lin, Jing Jer

AU - Huang, Hsu Shan

PY - 2012/4

Y1 - 2012/4

N2 - A series of symmetrical disubstituded 1,8-diamidoanthraquinones were synthesized and evaluated for anti-proliferation, telomerase inhibitory by TRAP assay, and hTERT expression by SEAP assay. All of the compounds tested, except for compounds 3a and 3s were selected by the NCI screening system. In addition, compounds 4e and 4k exhibited inhibitory effects on telomerase activity. Taken together, our findings indicated that the analysis of cytotoxicity and telomerase inhibition might provide information applicable for further developing potential telomerase targeting strategy.

AB - A series of symmetrical disubstituded 1,8-diamidoanthraquinones were synthesized and evaluated for anti-proliferation, telomerase inhibitory by TRAP assay, and hTERT expression by SEAP assay. All of the compounds tested, except for compounds 3a and 3s were selected by the NCI screening system. In addition, compounds 4e and 4k exhibited inhibitory effects on telomerase activity. Taken together, our findings indicated that the analysis of cytotoxicity and telomerase inhibition might provide information applicable for further developing potential telomerase targeting strategy.

KW - Amidoanthraquinones

KW - NCI 60-cell panel assay

KW - SEAP assay

KW - TRAP assay

KW - Telomerase

KW - hTERT expression

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Design, synthesis and evaluation of telomerase inhibitory, hTERT repressing, and anti-proliferation activities of symmetrical 1,8-disubstituted amidoanthraquinones

Abstract

Keywords

ASJC Scopus subject areas

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