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

20 引文 (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
47
發行號1
DOIs
出版狀態已發佈 - 一月 2012

指紋

Telomerase
Assays
Derivatives
Cell Line
Prostatic Neoplasms
Cells
Pharmaceutical Preparations
Neoplasms
Cytotoxicity

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

引用此文

Synthesis, antiproliferative activities and telomerase inhibition evaluation of novel asymmetrical 1,2-disubstituted amidoanthraquinone derivatives. / Lee, Chia Chung; Huang, Kuo Feng; Lin, Pen Yuan; Huang, Fong Chun; Chen, Chun Liang; Chen, Tsung Chih; Guh, Jih Hwa; Lin, Jing Jer; Huang, Hsu Shan.

於: European Journal of Medicinal Chemistry, 卷 47, 編號 1, 01.2012, p. 323-336.

研究成果: 雜誌貢獻文章

Lee, Chia Chung ; Huang, Kuo Feng ; Lin, Pen Yuan ; Huang, Fong Chun ; Chen, Chun Liang ; Chen, Tsung Chih ; Guh, Jih Hwa ; Lin, Jing Jer ; Huang, Hsu Shan. / Synthesis, antiproliferative activities and telomerase inhibition evaluation of novel asymmetrical 1,2-disubstituted amidoanthraquinone derivatives. 於: European Journal of Medicinal Chemistry. 2012 ; 卷 47, 編號 1. 頁 323-336.
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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.",
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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

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